Substituted semicarbazone arthropodicides

ABSTRACT

Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.

This is a division of application Ser. No. 07/689,042, filed May 20, 1991, now U.S. Pat. No. 5,182,303, which is a continuation-in-part of application Ser. No. 07/436,361, filed on Nov. 13, 1989, now abandoned, which was a continuation-in-part of U.S. Ser. No. 07/290,404, filed Dec. 27, 1988, now abandoned.

BACKGROUND OF THE INVENTION

U.S. Pat. No. 4,547,524 discloses benzoyl hydrazone derivatives as insecticides.

WO 8800197 discloses as part of a broader scope substituted semicarbazones derived from chromanones and thiochromanones as intermediates used in the preparation of insecticides.

EP-3,913 discloses substituted benzophenone hydrazones to be useful as insecticides.

EP-26,040 discloses a broad scope of substituted hydrazones to be useful as insecticides.

EP-254,461 discloses N-substituted hydrazones to be useful as insecticides.

GB-A-1,374,725 discloses structurally related semicarbazide insecticides.

J. Ind. Chem. Soc. 37, pages 443 to 50 (1960) discloses a compound of the formula: ##STR1## but no utility therefor.

SUMMARY OF THE INVENTION

This invention pertains to compounds of Formula I, including all geometric isomers, stereoisomers, and agronomically and nonagronomically suitable salts thereof, compositions containing them, and their use as agronomic and nonagronomic arthropodicides: ##STR2## wherein: Q is ##STR3## A is (CH₂)_(t), O, S(O)_(q), NR₇, OCH₂ or S(O)_(q) CH₂, wherein, each carbon individually can be substituted with 1 to 2 substituents selected from 1 to 2 halogen, C₁ -C₆ alkyl, C₃ -C₆ cycloalkyl, C₃ -C₆ halocycloalkyl, C₄ -C₇ alkylcycloalkyl, C₂ -C₄ alkoxycarbonyl, or phenyl optionally substituted with 1 to 3 substituent independently selected from W;

R₁ and R₂ are independently R₈, halogen, CN, NO₂, N₃, SCN, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, C(O)R₈, CO₂ R₈, C(O)NR₈ R₉, OC(O)R₈, OCO₂ R₈, OC(O)NR₈ R₉, NR₉ C(O)R₈, NR₉ C(O)NR₈ R₉, OSO₂ R₈, NR₉ SO₂ R₈, or when m is 2, R₁ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O OR CH₂ CH₂ O each of which is optionally substituted with 1 to 4 halogen atoms or 1 to 2 methyl groups, or when n is 2, R₂ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O or CH₂ CH₂ O each of which can be substituted 1 to 4 halogens or 1 to 2 methyl groups; R₂ being other than CH₃ when R₁, R₃ and R₄ are H and A is CH₂ ;

R₃ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₄ -C₆ alkylcycloalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylalkyl, OR₈, S(O)_(q) R₈, NR₈ R₉, CN, CO₂ R₈, C(O)R₈, C(O)NR₈ R₉, C(S)NR₈ R₉, C(S)R₈, C(S)SR₈, phenyl optionally substituted with (R₁₀)_(p) or benzyl optionally substituted with 1 to 3 substituents independently selected from W or R₃ is C₃ -C₆ cycloalkyl optionally substituted with 1 to 2 halogens or 1 to 2 CH₃ ;

R₄ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ cyanoalkyl, phenyl optionally substituted with (R₁₀)_(p) or benzyl optionally substituted with 1 to 3 substituents independently selected from W;

R₅ and R₆ are independently H, C₁ -C₂₂ alkyl, C₂ -C₂₂ alkoxyalkyl, C₂ -C₂₂ alkylcarbonyl, C₂ -C₂₂ alkoxycarbonyl, C₂ -C₂₂ haloalkyl carbonyl, C₂ -C₂₂ haloalkoxycarbonyl, SR₁₁, CHO, C₁ -C₄ alkylsulfonyl, phenylsulfonyl optionally substituted with 1 to 3 substituents independently selected from W; C₇ -C₁₅ phenoxycarbonyl optionally substituted with 1 to 3 substituents selected from W; C₇ -C₁₅ phenylcarbonyl optionally substituted with 1 to 3 substituents independently selected from W; C(O)CO₂ C₁ to C₄ alkyl, C₈ -C₁₂ benzyloxycarbonyl optionally substituted with 1 to 3 substituents independently selected from W; or R₅ and R₆ are independently phenyl optionally substituted with 1 to 3 substituents independently selected from W, or benzyl optionally substituted with 1 to 3 substituents independently selected from W;

R₇ is H, C₁ -C₄ alkyl or phenyl optionally substituted with W; SR₈, SOR₈, SO₂ R₈, C(O)R₈, CO₂ R₈, C(O)NR₈ R₉, C(S)NR₈ R₉, C(S)R₈, C(S)OR₈, P(O)(OR₈)2, P(S)(OR₈)2, P(O)(R₈)OR₈ or P(O)(R₈)SR₈ ; provided that when R₇ is other than COR₈, C(O)NR₈ R₉ or C(S)NR₈ R₉ then R₈ is other than H;

R₈ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₄ -C₇ cycloalkylalkyl halocycloalkylalkyl C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ alkylthioalkyl, C₁ -C₆ nitroalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₃ -C₆ cycloalkyl, C₃ -C₆ halocycloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W or benzyl optionally substituted with 1 to 3 substituents independently selected from W;

R₉ is H, C₁ -C₄ alkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, or R₈ and R₉ is optionally taken together as (CH₂)₄, (CH₂)₅ or (CH₂ CH₂ OCH₂ CH₂);

R₁₀ is R₈, halogen, CN, NO₂, N₃, SCN, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, COR₈, CO₂ R₈, CONR₈ R₉, SO₂ NR₈ R₉, OC(O)R₈, OCO₂ R₈, OC(O)NR₈ R₉, NR₉ C(O)R₈, NR₉ C(O)NR₈ R₉, OSO₂ R₈, NR₉ SO₂ R₈ or when p is 2, R₁₀ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O, or CH₂ CH₂ O each of which is optionally substituted with independently, 1 to 4 halogen atoms or 1 to 2 methyl groups;

R₁₁ is C₁ -C₂₂ alkyl, C₁ -C₂₂ haloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W, or R₁₁ is NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, NR₁₂ R₁₆, SR₁₄, ##STR4## R₁₂ and R₁₆ are independently selected from C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₃ -C₆ cycloalkyl, C₄ -C₇ cycloalkylalkyl, C₂ -C₆ cyanoalkyl, C₂ -C₆ alkoxyalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₄ -C₈ dialkylaminocarbonylalkyl, phenyl optionally substituted by 1 to 2 substituents selected from W, benzyl optionally substituted by 1 to 2 substituents selected from W and phenethyl optionally substituted by 1 to 2 substituents selected from W, or R₁₂ -R₁₆ is optionally taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂, each ring optionally substituted with 1 to 2 CH₃ ;

R₁₃ is F, C₁ -C₂₀ alkyl, C₁ -C₆ , haloalkyl, C₂ -C₈ dialkylamino, piperidinyl, pyrrolidinyl, morpholinyl, phenyl optionally substituted with 1 to 3 substituents selected from W, or R₁₃ is C₁ -C₂₀ alkoxy C₁ -C₆ haloalkoxy or C₁ -C₄ alkoxy substituted with cyano, nitro, C₁ -C₄ alkoxy, C₄ -C₈ alkoxyalkoxy, C₁ -C₂ alkylthio, C₂ -C₃ alkoxycarbonyl, C₃ -C₅ dialkylaminocarbonyl or phenyl optionally substituted with 1 to 3 substituents independently selected from W, or R₁₃ is phenoxy optionally substituted with 1 to 3 substituents selected from W;

R₁₄ and R₁₅ are independently selected from C₁ -C₄ alkyl, C₂ -C₄ haloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W or R₁₄ and R₁₅ is optionally taken together as (CH₂)₂, (CH₂)₃ or CH₂ C(CH₃)₂ CH₂ ;

W is halogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂ haloalkyl, C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl;

m is 1 to 5;

n is 1 to 4;

t is 0 to 3;

q is 0 to 2;

p is 1 to 3;

a is 0 to 2;

V is O or S;

X is O or S; X being O when A is CH₂ and R₂, R₃ and R₄ are H;

Y is O or S; and

Z is O or S.

Preferred Compounds (A) are those compounds of Formula I wherein;

when R₃ or R₄ is H and A is oxygen then the remaining R₃ or R₄ is other than phenyl or phenyl optionally substituted with W and when t is 0 then R₃ or R₄ are other than Ph or phenyl optionally substituted with W.

Preferred Compounds (B) are Compounds of Formula I wherein;

R₁, R₂ and R₁₀ are R₈, halogen, CN, NO₂, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, CO₂ R₈, SO₂ NR₈ R₉, or when m, n or q is 2, then R₁, R₂ or R₁₀ respectively is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O or CH₂ CH₂ O each of which is optionally substituted with 1 to 4 halogens or 1 to 2 methyl groups;

R₈ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₃ -C₆ cycloalkylalkyl, C₃ -C₆ halocycloalkylalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₃ -C₆ cycloalkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W or benzyl optionally substituted with 1 to 2 substituents independently selected from W;

R₅ and R₆ are independently H, C₁ -C₃ alkyl, C₂ -C₄ alkylcarbonyl, C₂ -C₄ alkoxycarbonyl, CHO, SR₁₁, phenyl optionally substituted with 1 to 2 substituents independently selected from W, or benzyl optionally substituted with 1 to 2 substituents independently selected from W;

R₁₁ is C₁ -C₃ alkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W, NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, NR₁₂ R₁₆ ; ##STR5## R₁₂ and R₁₆ are independently selected from C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₅ -C₆ cycloalkyl, C₃ -C₈ alkoxycarbonylalkyl, phenyl, benzyl and phenethyl or each phenyl, benzyl and phenethyl optionally substituted with 1 to 2 substituents independently selected from W, or R₁₂ and R₁₆ can be taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ;

R₁₄ and R₁₅ are independently selected from C₁ to C₃ a1ky1 or phenyl;

m is 1 to 2;

n is 1 to 2;

p is 1 to 2;

q is 0;

V is S; and

a is 2.

Preferred Compounds (C) are Compounds B wherein:

R₃ is H, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, CN, phenyl optionally substituted with (R₁₀)p or benzyl optionally substituted with 1 to 2 substituents independently selected from W;

R₄ is H, C₁ -C₃ alkyl, C₃ -C₄ alkenyl or C₃ -C₄ alkynyl;

R₅ is H, Me, CO₂ Me, CO₂ Et, SR₁₁ or phenyl optionally substituted with 1 to 2 substituents independently selected from W;

R₆ is H, Me, C(O)Me, CO₂ Me or SR₁₁ ;

R₁₁ is C₁ -C₃ alkyl, NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, or phenyl optionally substituted with Cl, NO₂ or CH₃ ;

R₁₂ is C₁ -C₄ alkyl or phenyl optionally substituted with Cl or CH₃ ;

R₁₃ is C₁ -C₁₂ alkyl, C₁ -C₁₂ alkoxy, C₁ -C₆ haloalkyl, dimethylamino, phenyl optionally substituted with Cl or CH₃, or R₁₃ is C₁ -C₄ alkoxy substituted with C₂ -C₄ alkoxy or 1 to 6 halogens;

A is CH₂, CH₂ CH₂, O, S, OCH₂, NR₇ or SCH₂, wherein, each carbon is optionally substituted with C₁ -C₃ alkyl or phenyl, wherein, the phenyl is optionally substituted with W; and;

R₇ is H, C₁ -C₄ alkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, C₂ -C₄ alkylcarbonyl, C₂ -C₄ alkoxycarbonyl or C₁ -C₄ alkylsulfonyl.

Preferred Compound (D) are Compounds C wherein:

R₁ and R₂ are independently selected from F, Cl, Br, CN, NO₂, OMe, CF₃, OCF₂ H, OCF₂ CF₂ H, SMe, SO₂ Me, SCF₂ H or when m or n is 2 R₁ or R₂ respectively is optionally taken together as CH₂ C(CH₃)2O or CF₂ CF₂ O;

R₃ is Cl to C₄ alkyl, allyl, propargyl, or phenyl optionally substituted with F, Cl, Br, CF₃, OCF₂ H, OCF₃, SCF₂ H, CN, NO₂, CH₃, OMe or CO₂ Me;

R₄ is H or CH₃ ;

R₅ is H, CH₃ CO₂ CH₃, CO₂ Et, or phenyl optionally substituted with F or Cl;

R₆ is H, CH₃, C(O)CH₃ or CO₂ CH₃ ; and

A is O, S or CH₂, optionally substituted with C₁ -C₃ alkyl or phenyl which may also be optionally substituted with W.

Preferred Compounds (E) are Compounds D wherein A is CH₂ ; and R₃ is optionally substituted phenyl or C₁ to C₄ alkyl. Preferred Compounds (F) are compounds of Formula I wherein Q is Q-1. Preferred Compounds (G) are compounds of Formula I wherein Q is Q-2. Preferred Compounds (H) are compounds of Formula I wherein Q is Q3 Preferred Compounds (I) are compounds of Formula I wherein Q is Q4. Preferred Compounds (J) are compounds of Formula I wherein Q is Q₅. Preferred Compounds (K) are compounds of Formula I wherein Q is Q6 Preferred Compounds (L) are compounds of Formula I wherein Q is Q₇. Preferred Compounds (M) are compounds of Formula I wherein Q is Q₈. Preferred Compounds (N) are Compounds (E) wherein Q is Q-1.

Specifically preferred are the compounds:

O) 2-[5-fluoro-2-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-yl-idene]-N-[4-(trifluoromethoxy)phenyl]hydrazine carboxamide;

P) 2-[6-chloro-2,3-dihydro-2-methyl-2-(2-propenyl)-3-benzo-furanylidene]-N-[4-(trifluoromethoxy)phenyl]hydrazine carboxamide;

Q) 2-(5-fluoro-2,3-dihydro-2-methyl -1H-inden-1-ylidene)-N-[4-(trifluoro methyl)phenyl]hydrazine carboxamide;

R) 2-[5-chloro-2,3-dihydro-2-(1-methylethyl) -1H-inden-1-ylidene]-N-[4-(trifluoromethyl)phenyl]hydrazine carboxamide;

S) 2-(5-chloro-2,3-dihydro-2-methyl-1H-inden-1-ylidene)-N-[4-(trifluoromethyl) phenyl]hydrazine carboxamide; and

T) 2-[5-fluoro-2-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-yl-idene]-N-[4-(trifluoromethyl)phenyl]hydrazine carboxamide.

DETAILS OF THE INVENTION

The compounds of Formula I, where Q is Q-1, can be prepared by the reaction of hydrazones of Formula II with an aryl isocyanate of Formula III. Compounds of Formula I, where Q is Q-2 through Q-8, can be prepared by procedures which are analogous to those for compounds where Q is Q-1; therefore, for brevity only the Q-1 compounds are described. Typical reactions involve combination of equimolar amounts of II and III in a suitable solvent at temperatures generally in the range of -10° to 100° C. Although the reaction can be run neat, a solvent is generally preferred. Suitable solvents typically have sufficient polarity to effect solution of the Formula II hydrazone and include, but are not limited to, ethers such as diethyl ether, tetrahydrofuran and dioxane; halogenated hydrocarbons such as methylene chloride, chloroform and carbon tetrachloride; aromatic hydrocarbons such as benzene, toluene and xylene; esters such as ethyl acetate and polar aprotic solvents such as dimethylformamide and dimethylacetamide. ##STR6##

Compounds of Formula I include both geometrical and optical isomers as well as syn and anti isomers around the nitrogen-nitrogen bond. These isomers may vary in their biological activity. In some instances, it may be desirable to obtain compounds which are geometrically and/or optically pure or which are enriched in one or more of the possible isomers. All such isomers are included within the scope of this invention.

For the sake of simplifying the description of this invention, the generic formula (Formula I) encompasses certain compounds that may have long term stability problems and/or are difficult to prepare. For example, when R₁ is an OCO₂ R₈ group and R₈ is hydrogen the R₁ substituent is OCO₂ H which will decompose to the corresponding phenol and carbon dioxide. Similarly, haloalkylamines when R₁ is NR₈ R₉ and R₈ is C₁ to C₆ haloalkyl are unstable when the halo substituent is directly adjacent to nitrogen. These generally decompose to the corresponding hydrogen halides and imine. These compounds, however, are relatively few; their identity would be obvious to one skilled in the art, and their excision from the scope would unduly complicate and lengthen the description of the invention.

The hydrazones of Formula II can be obtained by processes known in the art involving condensation of a ketone of Formula IV with either hydrazine or a substituted derivative thereof (Formula V). This reaction is typically conducted with equimolar amounts of IV and V although greater than stoichiometric amounts of hydrazine (V) can be used. Suitable solvents include the alcohols such as methanol, ethanol, propanol, butanol and the like at temperatures in the range of 0° to 150° C., with the reflux temperature of the solvent generally being a convenient reaction temperature. Acid catalysis can also be useful, particularly for some of the more sterically hindered Formula IV compounds. Typical acid catalysts include sulfuric, hydrochloric and p-toluene sulfonic acid. ##STR7##

An alternate process useful for the preparation of compounds of Formula I involves condensation of a phenyl substituted semicarbazide of Formula VI with a ketone of Formula III. Preferred conditions for this reaction include an acid catalyst such as hydrochloric, sulfuric or p-toluene sulfonic acid. Reaction temperatures can range from 0° to 150° C. with the reflux temperature cf the solvent used generally preferred. Suitable solvents include, but are not limited to, ethers such as tetrahydrofuran and dioxane; aromatic hydrocarbons such as benzene and toluene; and especially preferred are alcohols such as methanol, ethanol and isopropanol. ##STR8##

Compounds of Formula I where R₅ and R₆ are other than hydrogen can generally be prepared from the corresponding compounds where R₅ and R₆ are hydrogen by reaction with electrophilic reagents such as alkyl halides, acyl halides, alkyl chloroformates and sulfenyl halides. The use of a base is generally preferred in these reactions but is dependent upon the specific nature of the reactants. For example, when the electrophilic reagent is selected from an alkyl halide, acyl halide or alkyl chloroformate, then metal hydrides such as sodium hydride or potassium hydride in solvents such as tetrahydrofuran or dimethylformamide are preferred. When sulfenyl halides are used then amine bases such as triethylamine in solvents such as diethyl ether or tetrahydrofuran are generally preferred. Of course, many of the compounds where R₅ is other than H can also be prepared by use of the appropriate hydrazine V in Scheme 2. For example, methyl hydrazine and methyl carbazate will produce compounds where R₅ is methyl and carbomethoxy, respectively.

The starting ketones of Formula II are known or can be obtained by processes analogous to known ones. Those skilled in the art will recognize the Formula II compounds to include indanones, tetralones, chromanones, thiochromanones, benzofuran-3-ones, thiobenzofuran-3-ones, isochromanones, isothiochromanones and others.

The following Examples illustrate the invention.

EXAMPLE 1 Step A: 3-chloro-α-(4-chlorophenyl)benzenepropanoic acid

To a solution of 6.8 g (0.17 mol) of 60% sodium hydride in 150 ml of dimethylformamide under nitrogen was added 30.0 g (0.162 mol) of methyl 4-chlorophenylacetate dropwise such that hydrogen evolution was moderate and the temperature of the reaction was maintained at less than 50° C. Once hydrogen evolution had ceased, a solution of 3-chlorobenzylbromide in 30 ml of dimethylformamide was added very cautiously such that the reaction temperature was maintained at less than 60° C. The reaction was maintained at 50° to 60° C. with stirring overnight after which time it was partitioned between 5% aqueous NaHCO₃ and diethyl ether, the aqueous extracts were washed twice with ether and the combined organic extracts were then washed with water. The ether extracts were dried over MgSO₄, filtered and concentrated to afford 48.0 g of a brown oil.

The crude product was combined with 300 ml of methanol, 40 ml of water and 20 ml of 50% aqueous sodium hydroxide and refluxed overnight. After this time the reaction was concentrated and the crude residue partitioned between water and ether. The aqueous extracts were acidified with conc. hydrochloric acid and extracted several times with ether. The ether extracts were dried over MgSO₄, filtered and concentrated to 48.8 g of a yellow, oily solid.

¹ H NMR (CDCl₃) δ3.0 (dd, 1H), 3.3 (m, 1H), 3.84 (t, 1H), 6.77 (d, 1H), 6.9-7.4 (m).

Step B: 5-chloro-2-(4-chlorophenyl)-2,3-dihydro-1H-inden-1-one

The crude product from Step A was combined with 50 ml of thionyl chloride and then heated at reflux for 2 hours. Thionyl chloride was removed by concentration at reduced pressure and then the mixture was concentrated several times from carbon tetrachloride. The residue was combined with 200 ml of dichloroethane, cooled under nitrogen to 0° C., and 24.5 g of aluminum trichloride was then added. After stirring overnight the reaction was poured onto a mixture of ice in 1N hydrochloric acid, extracted three times with ether and chromatographed on silica gel (10% ethyl acetate/hexane) to afford 18.6 g of a yellow oily solid.

¹ H NMR (CDCl₃) 6 3.20 (dd, 1H), 3.68 (dd, 1H), 3.90 (dd, 1H), 6.9-7.6 (m), 7.75 (d, 1H).

Step C: 2-[5-chloro-2-(4-chlorophenyl)-2,3-dihydro 1H-inden-1-ylidene]-N-[4-(trifluoromethyl) phenyl]hydrazinecarboxamide

A mixture of 1.5 g of the indanone from Step B and 0.75 ml of hydrazine hydrate in 10 ml of ethanol was refluxed under N₂ overnight. The mixture was then partitioned between 5% NaHCO₃ and ether, the aqueous extracts were washed with chloroform and the combined chloroform/ether extracts were washed with water. The organic extracts were dried over magnesium sulfate and concentrated to 1.54 g of a yellow oil. To 0.45 g of this oil was added 10 ml of THF and 0.29 g of 4-trifluoromethylphenyl isocyanate. The mixture was then stirred under nitrogen overnight. Concentration at reduced pressure and then trituration with ether provided 0.27 g of the title compound as a yellow solid, m.p. 214° to 216° C.

¹ H NMR (CDCl₃) δ2.95 (dd, 1H), 3.74 (dd, 1H), 4.30 (dd, 1H), 7.1-7.8 (m), 8.33 (s, 1H); IR (nujol) 1680, 3190, 3360 cm⁻¹.

EXAMPLE 2 Step A: ethyl 2[5-fluoro-2-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-ylidene]hydrazine carboxylate

To a mixture of 1.5 g of 5-fluoro-2-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-one (prepared by a procedure analogous to Example 1, Step B) and 0.63 g of ethyl carbazate in 20 ml of methanol was added 1 drop of conc. H₂ SO₄ and the reaction was refluxed under nitrogen overnight. The reaction was then partitioned between ethyl acetate and 5% aqueous NaHCO₃, the aqueous extracts were washed with ethyl acetate and the combined organic extracts were dried over MgSO₄. Concentration of the organic extract afforded 1.9 g of a yellow oil, which was triturated with ether to afford 1.27 g of a white solid, m.p. 139°-141° C.

¹ H NMR (CDCl₃) δ1.26 (t, 3H), 2.91 (dd, 1H), 3.70 (dd, 1H), 4.2 (m, 3H), 6.9-7.3 (m, 6H), 7.52 (bs, 1H), 7.93 (dd, 1H).

Step B: ethyl 2-[5-fluoro-2-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-ylidene]-1-[[[4-(trifluoromethyl)phenyl]amino]carbonyl]hydrazine carboxylate

To a solution of 1.02 g of the ethyl carboxylate from Step A and 0.62 g of 4-trifluoromethylphenylisocyanate in 10 ml of THF was added 0.26 ml of triethylamine and the mixture was stirred under nitrogen overnight. The reaction was then partitioned between ethyl acetate and 5% aqueous NaHCO₃ and the aqueous extracts were washed twice with ethyl acetate. The organic extracts were dried over MgSO₄ and concentrated to 1.67 g of a yellow oil. Chromatography on silica gel afforded 0.37 g of a yellow solid m.p. 144-146.

¹ H NMR (CDCl₃) δ1.16 (t, 3H), 3.00 (dd, 1H), 3.65 (dd, 1H), 3.8-3.9 (m, 1H), 4.0-4.1 (m, 1H), 4.32 (dd, 1H), 6.85-7.2 (m, 6H), 7.60 (s, 4H), 8.05 (dd, 1H), 10.66 (s, 1H).

EXAMPLE 3 Step A: N-[4-trifluoromethyl)phenyl]hydrazine carboxamide

To a 0° C. solution of 10 ml of hydrazine hydrate and 75 ml of THF was added dropwise a solution of 6 g of 4-trifluoromethyl phenyl isocyanate in 20 ml of THF. After 1 hr TLC indicated the reaction was complete. The reaction was partitioned between ether and water, the ether extracts were washed twice with water, dried over MgSO₄, and concentrated to 6.34 g of a white solid, m.p. 168°-172° C.

¹ H NMR (CDCl₃) δ3.9 (bm, 2H), 6.1 (bs, 1H), 7.56 (d, 2H), 7.61 (d, 2H), 8.4 (bs, 1H).

Step B: methyl-5-chloro-2,3-dihydro-2-methyl-1-oxo-1H-indene-2-carboxylate

To a mixture of 8.0 g of 5-chloroindanone and 4.2 ml of dimethylcarbonate in 60 ml of THF was added 4.0 g of 60% NaH and the mixture was heated to reflux under N₂ overnight. After this time the reaction was cooled to room temperature and 4.0 ml of methyl iodide was added and the mixture was reheated to reflux overnight. The reaction was then cooled and partitioned between ether and 5% aqueous NaHCO₃ and the aqueous extracts were washed twice with ether. The combined aqueous extracts were dried over MgSO₄ and concentrated to 11.24 g of a brown oil. Chromatogrpahy on silica gel (10% ethyl acetate/hexane) afforded 4.25 g of the title compound as a brown oil.

1H NMR (CDCl₃) δ1.52 (s, 3H), 2.96 (d, 1H), 3.68 (s, 3H), 3.69 (d, 1H), 7.40 (d, 1H), 7.47 (s, 1H), 7.71 (d, 1H).

Step C: methyl 5-chloro-2,3-dihydro-2-methyl-1-[[[[4-(trifluoromethyl)phenyl]amino]carbonyl]hydrazine]-1H-indene-2-carboxylate

To a mixture of 0.92 g of the compound from Step A and 1.0 g of the compound from Step B in 10 ml of methanol was added 1 drop of conc. H₂ SO₄ and the mixture was heated to reflux under N₂ overnight. The reaction was then cooled to 0° C. and the precipitate filtered, rinsed with cold methanol and dried to 0.39 g of a brown solid, m.p. 192°-194° C.

1H NMR (CDCl₃) 6 1.70 (s, 3H), 3.00 (d, 1H), 3.82 (s, 3H), 3.87 (d, 1H), 7.3 (m, 2H), 7.6-7.8 (m, 5H), 8.38 (s, 1H), 8.98 (s, 1H).

EXAMPLE 4 Step A: 3-(4-fluorophenyl)-1-phenyl-2-propen-1-one

To a mechanically stirred solution of 5.0 g NaOH in 35 ml H₂ O and 25 ml EtOH at 15° C. was added 12.0 g (0.100 mole) of acetophenone and 12.4 g (0.100 mole) of 4-fluorobenzaldehyde. After a brief exotherm to 25° C., the temperature returned to 15° C., and the cooling bath was removed. The reaction mixture was stirred at room temperature for 1.5 hour, and the thick slurry was transferred to a beaker to cool overnight at 10° C. This mixture was filtered, and the solids were washed with distilled H₂ O until the washings were neutral to litmus. Upon drying in vacuo, 20.8 g of a pale yellow solid was obtained, m.p. 86°-87° C.

IR (Nujol): 1660, 1605, 1590, 1580 cm⁻¹.

1H NMR (200 MHz, CDCl₃): δ7.12 (d, J=16 Hz, 1H), 7.42-7.68 (m, 7H), 7.78 (d, J=16 Hz, 1H), 8.02 (m, 2H).

Step B: 3-(4-fluorophenyl)-2,3-dihydro-1H-indene-1-one

The title compound of Step A, Example 4, 11.3 g (0.50 mole), was added to 250 ml of mechanically-stirred polyphosphoric acid at 135° C., under a nitrogen atmosphere. This mixture was heated at 135° C. for 2 hours and then allowed to cool to 90° C. Ice water was added at such a rate as to maintain a temperature below 125° C. Once the material had become fluid, it was poured over ice and extracted with ether. The ether extracts were washed twice with saturated aqueous NaHCO₃ and once with brine. The ethereal solution was dried over MgSO₄ and concentrated at reduced pressure. The resultant residue was recrystallized from hexane/chlorobutane to afford 5.90 g of the title compound as a brown powder, m.p. 117°-120° C.

IR (Nujol): 1705 (s), 1600 (br, m).

1H NMR (200 MHz, CDCl₃): 6 2.64 (dd, 1H), 3.22 (dd, 1H), 4.57 (dd, 1H), 6.96-7.15 (m, 4H), 7.25 (m, 1H), 7.44 (m, 1H), 7.58 (m, 1H), 7.81 (m, 1H).

Step C: 2-[3-(4-fluorophenyl)-2,3-dihydro-1H-inden-1-ylidene]-N-[4-(trifluoromethyl)phenyl]hydrazine carboxamide

The title compound of Step B, Example 4, 2.26 g (0.010 mole), was combined with 0.60 ml of hydrazine monohydrate (0.012 mole) in 30 ml of methanol and heated at reflux for 2 to 2.5 hours. The reaction mixture was concentrated at reduced pressure, and the resultant residue was dissolved in ethyl acetate and washed with saturated aqueous NaHCO₃, H₂ O, and brine. The organic phase was dried over MgSO₄ and concentrated in vacuo to afford 2.37 g of crude material. This material was dissolved in 30 ml of dry THF, and a 10 ml aliquot of this solution was added to a solution of 0.62 g (0.0033 mole) of 4-(trifluoromethyl)phenyl isocyanate in 20 ml of dry THF. After this mixture was stirred overnight under a nitrogen atmosphere, it was concentrated in vacuo. The resultant residue was triturated with hexanes and filtered to obtain 1.23 g of an off-white product, m.p. 253°-255° C.

1H), 4.65 (dd, 1H), 7.0-7.16 (m, 5H), 7.33-7.37 (m, 2H), 7.63-7.67 (m, 2H), 7.91-7.95 (m, 2H), 8.08 (m, 1H), 9.30 (s, NH), 10.00 (s, NH).

EXAMPLE 5 Step A: ethyl 4-fluoro-α-methylenebenzeneacetate

Sodium ethoxide solution was prepared by portionwise addition of sodium pieces (1.5 g, 0.065 mol) to ethanol (50 ml). To this solution was added first, 8.9 ml (0.065 mol) of diethyloxalate in one portion and second, 10 g (0.059 mol) of methyl 4-fluorobenzeneacetate dropwise at such a rate as to keep the reaction mixture at 25° C. After stirring at room temperature for 2 hrs, the ethanol was concentrated and the residue taken up in toluene. The toluene solution was concentrated and the solid residue was taken up in ether and 10% aqueous acetic acid. After stirring at room temperature for 1 hr the mixture was separated and the aqueous phase extracted twice with ether. The combined ether phases were washed once with saturated aqueous NaHCO₃ solution, dried (MgSO₄), and concentrated. The NMR of the crude product was complicated by a mixture of methyl and ethyl esters.

The crude diester was combined with 25 ml of water and 8 ml of 37% formalin solution. To this somewhat heterogeneous mixture was added a solution of 6.5 g of K₂ CO₃ in 36 ml of water, dropwise as such a rate as to maintain a temperature of about 25° C. The reaction was stirred vigorously for three hours to mix the fine emulsion. Ether was added and the aqueous phase was separated and extracted three times with ether. The combined ether phases were dried (MgSO₄) and concentrated to a colorless oil (11 g, 96% yield).

¹ H NMR (CDCl₃) δ: 7.41 (2H, m), 7.03 (2H, m), 6.34 (1H, s), 5.85 (1H, s), 4.28 (2H, q, J=7 Hz), 1.32 (3H, t, J=7 Hz).

Step B: ethyl 4-fluoro-α-[[(2-fluorophenyl)thiolmethyl]benzeneacetate

The crude product from Step A (3.9 g, 20 mmole) was taken up in 20 ml of ethanol. To this solution, being stirred at room temperature, was added 2-fluorothiophenol (2.5 g, 20 mmole) and 50 mg of solid sodium ethoxide. After stirring for eight hours the ethanol was concentrated and the residue taken up in ether. The ether mixture was washed twice with 15% NaOH solution, dried (MgSO₄) and concentrated to a colorless oil (5.3 g, 82% yield). 1H NMR (CDCl₃) δ: 7.28 (4H, m), 7.06 (4H, m), 4.13 (2H, m), 3.72 (1H, m), 3.55 (1H, m), 3.20 (1H, dd, J=6, 12 Hz), 1.21 (3H, t, J=6 Hz).

Step C: 4-fluoro-α-[[(2-fluorophenyl)thio]methyl]benzeneacetic acid

The crude ester from Step B (5.3 g, 16 mmole) was combined with 20 ml of 88% formic acid and 2.1 ml (33 mmole) of methane sulfonic acid. The emulsion was refluxed for five hours during which time it gradually became homogeneous. After cooling, water and methylene chloride were added and the aqueous phase was separated and extracted twice with methylene chloride. The organic phases were combined, dried (MgSO₄) and concentrated. The crude residue was taken up in 4% ethyl acetate/hexane and filtered through a plug of silica gel to remove nonpolar impurities. The product acid was then rinsed from the silica gel with ethyl acetate and the solvent concentrated. The acid was a colorless solid (4.5 g, 95% yield).

1H NMR (CDCl₃) δ: 10.05 (1H, br s), 7.20 (5H, m), 7.03 (3H, m), 3.81 (1H, dd, J=6, 8 Hz), 3.57 (1H, m), 3.23 (1H, dd, J=6, 12 Hz).

Step D: 8-fluoro-3-(4-fluorophenyl)-2.3-dihydro-4H-1-benzothiopyran-4-one

The acid from Step C (4.5 g, 15 mmole) was dissolved in 30 ml of thionyl chloride and refluxed for four hours. After cooling the thionyl chloride was concentrated and the residue taken up in carbon tetrachloride. The carbon tetrachloride was concentrated and the residue was taken up in 30 ml of dichloroethane. To the dichloroethane solution being cooled in an ice bath, was added aluminum trichloride (total of 2.1 g, 16 mmole) in three portions every 15 min. After stirring the black solution for an additional 30 min at 0° C., a 5% aqueous HCl solution was added. The aqueous phase was separated and extracted twice with methylene chloride. The organic phases were combined, dried (MgSO₄), and concentrated to give the crude product as a yellow oil (3.4 g, 82% yield).

1H NMR (CDCl₃) δ: 7.97 (1H, dd, J=3, 9 Hz), 7.19 (6H, m), 4.12 (1H, dd, J=4, 12 Hz), 3.58 (1H, m), 3.32 (1H, ddm J=4, 12 Hz).

Step E: 2-[8-fluoro-3-(4-fluorophenyl)-3,4-dihydro-2H-1-benzothiopyran-4-ylidene]-N-[4-(trifluoromethyl)phenyl]-hydrazinecarboxamide

The thiochromanone from Step D (1.1 g, 4.0 mmole) was treated according to the procedure in Example 1 Step C to give the desired product as a white powder (0.32 g, 17% yield). m.p.=217°-219° C. 1H NMR (CDCl₃) δ: 8.33 (1H, s), 7.98 (1H, d, J=9 Hz), 7.69 (1H, s) 7.60 (4H, AB, J_(AB) =8 Hz), 7.15 (6H, m), 4.42 (1H, t, J=4 Hz), 3.44 (1H, dd, J=4, 12 Hz), 2.99 (1H, dd, J=4, 12 Hz).

EXAMPLE 6 Step A: methyl 6-fluoro-1,2,3,4-tetrahydro-1-oxo-2-naphthalenecarboxylate

Hexane washed sodium hydride (3.5 g of 60%, 88 mmole) was covered with 75 ml of tetrahydrofuran and 5.4 ml (64 mmole) of dimethylcarbonate was added in one portion. The solution was heated to reflux and 6-fluoro-3,4-dihydro-1(2H)-naphthlenone (7.2 g, 44 mmole) in 25 ml of tetrahydrofuran was added dropwise while maintaining reflux. After the addition was complete, the reaction was refluxed for 1.5 hours. The reaction was then cooled in an ice bath and 10% aqueous HCl solution was carefully added. The solution was diluted with ether and the aqueous phase was separated and extracted twice with ether. The combined organic phases were dried (MgSO₄) and concentrated. The crude product was a pale yellow solid (9.6 g, 98% yield).

1H NMR (CDCl₃) δ: 7.99 (1H, dd, J=6,8 Hz), 6.95 (2H, m) 3.83 (3H, s), 3.82 (1H, m), 2.81 (2H, m), 2.58 (2H, m). NMR complicated by signals from enol tautomer.

Step B: methyl 6-fluoro-1,2,3,4-tetrahydro-1-oxo-2-phenyl-2-naphthalenecarboxylate

The tetralone from Step A (2.4 g, 10.8 mmole) and triphenylbismuth dichloride (5.8 g, 11.3 mmmole) were dissolved in 50 ml of benzene. 1,8-Diazabicyclo[5.4.0]-undec-7-ene (1.8 ml, 11.8 mmole) was added and the pale yellow solution was heated at reflux for 12 hours. The benzene solution was decanted from the gray sludge. The sludge was in turn triturated twice with ether and twice with acetone. The combined benzene, ether, and acetone phases were washed once with water, dried (MgSO₄), and concentrated. The resulting residue was flash chromatographed on silica gel eluting with 10% acetone/hexane. Purified product was obtained in 90% yield (2.9 g) as a viscous oil which solidified on standing.

1H NMR (CDCl₃) δ: 8.17 (1H, dd, J=8,10 Hz), 7.31 (5H, m) 7.02 (1H, dt, J=3,8 Hz), 6.85 (1H, dd, J=3,9 Hz), 3.75 (3H, s), 2.94 (2H, m), 2.89 (2H, m).

Step C: 6-fluoro-3,4-dihydro-2-phenyl-1(2H)-naphthalenone

The tetralone from Step B (2.8 g, 9.4 mmole) was dissolved in 45 ml of dimethylformamide. To this solution was added lithium chloride (2.0 g, 47 mmole) and water (0.42 ml, 23 mmole). The reaction mixture was heated to 150° C. for 2.5 hrs and then cooled and partitioned between ether and water. The aqueous phase was separated and extracted three times with ether. The combined organic phases were washed once with water, dried (MgSO₄), and concentrated (1.96 g, 87% yield).

1H NMR (CDCl₃) δ: 8.13 (1H, dd, J=6,10 Hz), 7.31 (5H, m) 6.99 (2H, m), 3.80 (1H, m), 3.07 (2H, m), 2.43 (2H, m).

Step D: 2-(6-fluoro-1,2,3,4-tetrahydro-2-phenyl-1-naphthalenylidene)-N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide

The crude product from Step C (0.65 g, 2.7 mmole) was treated according to the procedure in Example 1, Step C. The product was obtained as a white powder (0.26 g, 22% yield). m.p.=158°-160° C.

1H NMR (CDCl₃) δ: 8.45 (1H, s), 8.15 (1H, d, J=9 Hz), 7.98 (1H, s), 7.61 (5H, m), 7.29 (2H, m), 7.18 (2H, m), 6.92 (1H, dd, J=3,9 Hz), 6.75 (1H, d, J=3 Hz), 4.18 (1H, m), 2.64 (2H, m), 2.31 (1H, m), 2.10 (1H, m).

EXAMPLE 7 Step A: 4-Chloro-2-(2-methoxy-1-methyl-2-oxoethoxy)benzoic acid, methyl ester

A solution of methyl 4-chlorosalicylate (5.0 g) in dimethylformamide (10 ml) was treated sequentially with methyl 3-bromopropionate (4.0 g) and potassium carbonate (6.0 g). The mixture was stirred at room temperature for 18 hrs and diluted with water. The mixture was extracted with ether and the organics were washed with water. The organic layer was dried and evaporated to give the desired material (6.7 g) as a low melting solid.

NMR: 7.8 (d, 1H), 7.2 (m 1H), 6.9 (m, 1H), 4.8 (q, 1H), 3.9 (s, 3H), 3.8 (s, 3H), 1.7 (d, 3H).

Step B: 6-chloro-2-methyl-3(2H)-benzofuranone

A mixture of the compound of Example 7, Step A, (6.7 g) and sodium hydride (60% in oil, 1.5 g) was heated to reflux in tetrahydrofuran (50 ml). It was then allowed to cool to room temperature over 1.5 hrs. The cooled mixture was treated with aqueous ammonium chloride solution and ether. The ether solution was dried over magnesium sulfate and then evaporated. The oil was subjected to chromatography on silica gel with hexanes/ethyl acetate (25:1) as the eluent. The desired product (1.99 g) was obtained as a low melting solid.

NMR: 7.6 (d, 1H), 7.1 (m 2H), 4.7 (q, 1H), 1.55 (d, 3H).

Step C: (Z)-2-(6-chloro-2-methyl-3(2H)-benzofuranylidene)-N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide

The compound of Example 7, Step B, (1.9 g) was dissolved in ethanol (15 ml) and degassed with nitrogen. Then hydrazine hydrate (1.2 ml) was added and the mixture was heated at reflux for 1.5 hrs and evaporated to dryness. The residue was chromatographed on silica in hexanes/ethyl acetate (2:1). The first product eluted was the hydrazone syn to the methyl group (0.5 g). The next fraction (0.9 g) was mixed syn and anti. Pure anti hydrazone was eluted last (0.5 g). The syn hydrazone was treated with p-trifluoromethylphenylisocyanate (0.4 ml) in ether (10 ml). The desired material began to crystallize soon after mixing. The mixture was filtered and washed with ether to provide a solid (0.8 g). m.p.: 196°-198° C. NMR: 10.0 (br, 1H), 9.4 (br, 1H), 8.2-7.0 (m, 7H), 5.35 (m, 1H), 1.6 (d, 3H).

Step D: (E)-2-(6-chloro-2-methyl-3(2H)-benzofuranylidene)-N-[4-(trifluoromethyl)phenyl)hydrazinecarboxamide

Treating the anti hydrazone (0.5 g) obtained in Step C with p-trifluoromethylphenylisocyanate (0.4 ml) in the same manner as in Step C resulted in the isolation of the desired product as a solid (0.8 g). m.p.=205°-207° C. NMR: (10.4 (br, NH), 9.4 (br, 1H), 8.2-7.0 (m, 7H), 5.8 (m, 1H), 1.47 (d, 3H).

By the general procedures described herein and obvious modifications known to one skilled in the art, one can prepare the compounds of Tables 1 to 16. The compounds of Tables 1 through 10 are listed along with their melting points.

In Tables 1 through 16 the following notations have been used: ##STR9##

                                      TABLE 1                                      __________________________________________________________________________     (A = CH.sub.2, X = O)                                                          CMPD                                                                               R.sub.1                                                                             R.sub.2                                                                               R.sub.3                                                                               R.sub.4                                                                              R.sub.5                                                                             R.sub.6                                                                          m.p. °C.                            __________________________________________________________________________      1  4-CF.sub.3                                                                          5-Cl   4-ClPh H     H    H 214-216                                     2  4-Br 5-Cl   4-ClPh H     H    H 230-232                                     3  4-OMe                                                                               5-Cl   4-ClPh H     H    H 202-204                                     4  4-Cl 5-Cl   4-ClPh H     H    H 231-233                                     5  4-CF.sub.3                                                                          5-Cl   Ph     H     H    H 226-228                                     6  4-Br 5-Cl   Ph     H     H    H 237-238                                     7  4-OCF.sub.3                                                                         5-Cl   Ph     H     H    H 198- 200                                    8  4-CF.sub.3                                                                          5-Cl   4-FPh  H     H    H 223-225                                     9  4-Cl 5-Cl   4-FPh  H     H    H 224-226                                    10  4-Br 5-Cl   4-FPh  H     H    H 230-232                                    11  4-CF.sub.3                                                                          5-F    4-ClPh H     H    H 214-216                                    12  4-Cl 5-F    4-ClPh H     H    H 218-220                                    13  4-Br 5-F    4-ClPh H     H    H 223-225                                    14  4-CF.sub.3                                                                          5-F    4-FPh  H     H    H 224-226                                    15  4-Cl 5-F    4-FPh  H     H    H 212-214                                    16  4-Br 5-F    4-FPh  H     H    H 219-221                                    17  4-OCF.sub.3                                                                         5-F    4-FPh  H     H    H 201-203                                    18  4-CF.sub.3                                                                          5-F    Ph     H     H    H 230-232                                    19  4-Cl 5-F    Ph     H     H    H 233-235                                    20  4-Br 5-F    Ph     H     H    H 236-238                                    21  4-OCF.sub.3                                                                         5-F    Ph     H     H    H 187-190                                    22  4-CF.sub.3                                                                          5-OMe  Ph     H     H    H 219-221                                    23  4-OCF.sub.3                                                                         5-OMe  Ph     H     H    H 189-191                                    24  4-CF.sub.3                                                                          5-OMe  4-FPh  H     H    H 197-199                                    25  4-CF.sub.3                                                                          5-OCH.sub.2 CF.sub.3                                                                  4-FPh  H     H    H 217-219                                    26  4-OCF.sub.3                                                                         4-OCH.sub.2 CF.sub.3                                                                  4-FPh  H     H    H 204-206                                    27  4-CF.sub.3                                                                          5-O-i-Pr                                                                              4-FPh  H     H    H 198-201                                    28  4-CF.sub.3                                                                          4-OPh  4-FPh  H     H    H 224-226                                    29  4-CF.sub.3                                                                          5-OEt  4-FPh  H     H    H 206-208                                    30  4-OCF.sub.3                                                                         5-OEt  4-FPh  H     H    H 195-197                                    31  4-Cl H      Ph     H     H    H 220-221                                    32  4-Br H      Ph     H     H    H 231-232                                    33  4-CF.sub.3                                                                          H      Ph     H     H    H 223-224                                    34  4-Cl H      4-FPh  H     H    H 197-201                                    35  4-CF.sub.3                                                                          5-OH   Ph     H     H    H 240-242                                    36  4-CF.sub.3                                                                          5-Br   4-FPh  H     H    H 218-220                                    37  4-Br 5-Br   4-FPh  H     H    H 227-229                                    38  4-CF.sub.3                                                                          5-F    3-CF.sub.3Ph                                                                          H     H    H 225-227                                    39  4-Br 5-F    3-CF.sub.3Ph                                                                          H     H    H 221-223                                    40  4-CF.sub.3                                                                          5-F    2-FPh  H     H    H 218-220                                    41  4-Br 5-F    2-FPh  H     H    H 231-233                                    42  4-CF.sub.3                                                                          5-F    3-FPh  H     H    H 210-212                                    43  4-Br 5-F    3-FPh  H     H    H 218-220                                    44  4-CF.sub.3                                                                          5-F    2,4-di-FPh                                                                            H     H    H 219-221                                    45  4-Br 5-F    2,4-di-FPh                                                                            H     H    H 214-216                                    46  4-CF.sub.3                                                                          5-F    4-OEtPh                                                                               H     H    H 184-186                                    47  4-CF.sub.3                                                                          5-F    4-MePh H     H    H 219-221                                    48  4-Br 5-F    4-MePh H     H    H 227-229                                    49  4-CF.sub.3                                                                          5-F    2-naphthyl                                                                            H     H    H 229-230                                    50  4-Br 5-F    2-naphthyl                                                                            H     H    H 230-232                                    51  4-CF.sub.3                                                                          5-F    3,4-di-ClPh                                                                           H     H    H 214-216                                    52  4-CF.sub.3                                                                          4-F    Ph     H     H    H 214-216                                    53  4-Br 4-F    Ph     H     H    H 222-224                                    54  4-CF.sub.3                                                                          4-F    4-ClPh H     H    H 236-238                                    55  4-OCF.sub.3                                                                         4-F    4-ClPh H     H    H 209-211                                    56  2,4-di-Cl                                                                           5-Cl   Ph     H     H    H >250                                       57  H    5-Cl   Ph     H     H    H 209-211                                    58  4-NO.sub.2                                                                          5-Cl   Ph     H     H    H >250                                       59  3,4-di-Cl                                                                           5-F    4-FPh  H     H    H 132-136                                    60  2,4-di-F                                                                            5-F    4-FPh  H     H    H 213-215                                    61  4-F  5-F    4-FPh  H     H    H 216-218                                    62  4-CF.sub.3                                                                          6-F    4-ClPh H     H    H 237-239                                    63  4-Cl 6-F    4-ClPh H     H    H 236-238                                    64  4-Br 6-F    4-ClPh H     H    H 238-240                                    65  4-CF.sub.3                                                                          7-Cl   Ph     H     H    H 124-125                                    66  4-CF.sub.3                                                                          4,5-di-F                                                                              4-FPh  H     H    H 233-235                                    67  4-OCF.sub.3                                                                         4,5-di-F                                                                              4-FPh  H     H    H 224-226                                    68  4-Br 4,5-di-F                                                                              4-FPh  H     H    H 229-231                                    69  4-CF.sub.3                                                                          5-Cl   4-ClPh Me    H    H 165-169                                    70  4-Br 5-Cl   4-ClPh Me    H    H 149-153                                    71  4-OMe                                                                               5-Cl   4-ClPh Me    H    H 187-190                                    72  4-CF.sub.3                                                                          5-F    4-FPh  Me    H    H 85-89                                      73  4-Br 5-F    4-FPh  Me    H    H 70-74                                      74  4-CF.sub.3                                                                          5-Cl   H      H     H    H 240-242                                    75  4-Br 5-Cl   H      H     H    H 244-246                                    76  4-Cl 5-Cl   H      H     H    H 248-249                                    77  4-CF.sub.3                                                                          5-Cl   Me     H     H    H 208-210                                    78  4-Cl 5-Cl   Me     H     H    H 221-223                                    79  4-Br 5-Cl   Me     H     H    H 228-230                                    80  4-CF.sub.3                                                                          7-Cl   Me     H     H    H >250                                       81  4-CF.sub.3                                                                          5-F    Me     H     H    H 218-220                                    82  4-Cl 5-F    Me     H     H    H 219-221                                    83  4-Br 5-F    Me     H     H    H 224-226                                    84  4-CF.sub.3                                                                          4-OMe  Et     H     H    H 191-193                                    85  4-OCF.sub.3                                                                         5-OMe  Et     H     H    H 178-180                                    86  4-CF.sub.3                                                                          5-Cl   CO.sub.2 Me                                                                           H     H    H 242-244                                    87  4-CF.sub.3                                                                          5-F    CO.sub.2 Me                                                                           H     H    H 238-240                                    88  4-CF.sub.3                                                                          5-Cl   CO.sub.2 Me                                                                           Me    H    H 192-194                                    89  4-CF.sub.3                                                                          5-F    CO.sub.2 Me                                                                           Me    H    H 203-205                                    90  4-CF.sub.3                                                                          5-Cl   i-Pr   H     H    H 216-218                                    91  4-OCF.sub.3                                                                         5-Cl   i-Pr   Me    H    H 204-206                                    92  4-CF.sub.3                                                                          5-OCH.sub.2 CF.sub.3                                                                  Me     H     H    H 212-214                                    93  4-OCF.sub.3                                                                         5-OCH.sub.2 CF.sub.3                                                                  Me     H     H    H 189-191                                    94  4-Cl 4-OCH.sub.2 CF.sub.3                                                                  Me     H     H    H 220-222                                    95  4-CF.sub.3                                                                          5-Cl   Me     Me    H    H 215-217                                    96  4-Br 5-Cl   Me     Me    H    H 214-216                                    97  4-Cl 5-Cl   Me     Me    H    H 203-205                                    98  5-CF.sub.3                                                                          5-F    i-Pr   H     H    H 216-220                                    99  4-Br 5-F    i-Pr   H     H    H 217-222                                    100 4-CF.sub.3                                                                          5-F    H      H     H    H >245                                       101 4-Cl 5-F    H      H     H    H 240-242                                    102 4-Br 5-F    H      H     H    H >245                                       103 4-CF.sub.3                                                                          5-F    4-FPh  H     C(O)Me                                                                              H oil                                        104 4-OCF.sub.3                                                                         5-F    4-FPh  H     C(O)Me                                                                              H oil                                        105 4-CF.sub.3                                                                          5-F    4-FPh  H     CO.sub.2 Me                                                                         H oil                                        106 4-CF.sub.3                                                                          5-F    2,4-di-Ph                                                                             H     CO.sub.2 Me                                                                         H oily                                                                           solid                                      107 4-CF.sub.3                                                                          5-F    4-FPh  H     CO.sub.2 Et                                                                         H 144-146                                    108 4-Br H      4-FPh  H     H    H 204-207                                    109 4-CF.sub.3                                                                          H      4-FPh  H     H    H 212-213                                    110 4-Cl 4-Cl   Ph     H     H    H 234-239                                    111 4-Br 4-Cl   Ph     H     H    H 283-285                                    112 4-CF.sub.3                                                                          4-Cl   Ph     H     H    H 205-209                                    113 4-CF.sub.3                                                                          5-Me   4-ClPh H     H    H 210-214                                    114 4-Br 5-Me   4-ClPh H     H    H 260-262                                    115 4-Cl 5-Me   4-ClPh H     H    H 270-272                                    116 4-CF.sub.3                                                                          4-Cl   4-FPh  H     H    H wax                                        117 4-Br 4-Cl   4-FPh  H     H    H wax                                        118 4-Cl 4-Cl   4-FPh  H     H    H wax                                        119 4-CF.sub.3                                                                          5-F    CH.sub.2 Ph-4-F                                                                       CH.sub.2 Ph-4-F                                                                      H    H 76-81                                      120 4-Cl 5-F    CH.sub.2 Ph-4-F                                                                       CH.sub.2 Ph-4-F                                                                      H    H 84-89                                      __________________________________________________________________________

                  TABLE 2                                                          ______________________________________                                          ##STR10##                                                                     (A = CH.sub.2 CH.sub.2, X = O)                                                 CMPD  R.sub.1  R.sub.2                                                                               R.sub.3  R.sub.4                                                                            R.sub.5                                                                             R.sub.6                                                                            m.p. °C.                    ______________________________________                                         121   4-Br     5-Cl   Ph       H   H    H   209-210                            122   4-CF.sub.3                                                                              5-Cl   Ph       H   H    H   217-218                            123   4-Cl     5-Cl   4-BrPh   H   H    H   236-238                            124   4-Br     5-Cl   4-BrPh   H   H    H   248-250                            125   4-CF.sub.3                                                                              5-Cl   4-BrPh   H   H    H   245-247                            126   4-Cl     5-Cl   4-OMePh  H   H    H   209-210                            127   4-Br     5-Cl   4-OMePh  H   H    H   216-217                            128   4-CF.sub.3                                                                              5-Cl   4-OMePh  H   H    H   226-228                            129   4-Cl     5-Cl   Me       H   H    H   236-238                            130   4-Br     5-Cl   Me       H   H    H   230-235                            131   4-CF.sub.3                                                                              5-Cl   Me       H   H    H   234-235                            132   4-CF.sub.3                                                                              5-Cl   CO.sub.2 Me                                                                             H   H    H   220-222                            133   4-Br     5-Cl   4-FPh    H   H    H   221-222                            134   4-CF.sub.3                                                                              5-Cl   4-FPh    H   H    H   233-234                            135   4-CF.sub.3                                                                              5-Cl   H        H   Me   H   114-117                            136   4-Cl     4-F    Me       H   H    H   233-236                            137   4-Br     4-F    Me       H   H    H   236-239                            138   4-CF.sub.3                                                                              4-F    Me       H   H    H   235-237                            139   4-Cl     5-F    Ph       H   H    H   179-184                            140   4-Br     5-F    Ph       H   H    H   185-192                            141   4-CF.sub.3                                                                              5-F    Ph       H   H    H   158-160                            142   4-CF.sub.3                                                                              4-F    CO.sub.2 Me                                                                             H   H    H   203-204                            143   4-CF.sub.3                                                                              5-F    4-FPh    H   H    H   179-180                            144   4-CF.sub.3                                                                              5-F    4-ClPh   H   H    H   225-230                            145   4-Cl     5-F    Me       H   H    H   200-210                            146   4-Br     5-F    Me       H   H    H   196-198                            147   4-CF.sub.3                                                                              5-F    Me       H   H    H   195-198                            148   4-CF.sub.3                                                                              H      CO.sub.2 Me                                                                             H   H    H   207-208                            149   4-CF.sub.3                                                                              H      CO.sub.2 Me                                                                             H   Me   H   oil                                150   4-CF.sub.3                                                                              H      H        H   H    H   230-232                            151   4-CF.sub.3                                                                              H      4-ClPh   H   H    H   228-230                            152   4-OMe    H      4-ClPh   H   H    H   191-193                            153   4-F      H      4-ClPh   H   H    H   204-205                            154   3-CF.sub.3                                                                              H      4-ClPh   H   H    H   199-200                            155   3-CO.sub.2 Et                                                                           H      4-ClPh   H   H    H   205-206                            156   4-F, 3-Cl                                                                               H      4-ClPh   H   H    H   210-212                            157   4-CF.sub.3                                                                              5-Br   H        H   H    H   253-255                            158   4-CF.sub.3                                                                              5-F    H        H   H    H   257-259                            ______________________________________                                    

                  TABLE 3                                                          ______________________________________                                          ##STR11##                                                                     (A = (CH.sub.2).sub.3, X = O)                                                  CMPD  R.sub.1  R.sub.2 R.sub.3                                                                              R.sub.4                                                                             R.sub.5                                                                             R.sub.6                                                                             m.p. °C.                    ______________________________________                                         159   4-CF.sub.3                                                                              5-Cl    H     H    H    H    224-225                            160   4-Cl     5-Cl    H     H    H    H    211-213                            161   4-Br     5-Cl    H     H    H    H    210-213                            162   4-CF.sub.3                                                                              5-Cl    Me    H    H    H    174-176                            ______________________________________                                    

                                      TABLE 4                                      __________________________________________________________________________      ##STR12##                                                                     (X = O)                                                                        CMPD                                                                               R.sub.1                                                                             R.sub.2                                                                            R.sub.3                                                                            R.sub.4                                                                             R.sub.5                                                                            R.sub.6                                                                           A  m.p. °C.                                __________________________________________________________________________     163 4-Cl H   Me  Me   H   H  O  177-182                                        164 4-CF.sub.3                                                                          H   Me  Me   H   H  O  186-188                                        165 4-CF.sub.3                                                                          5-Cl                                                                               Me  Me   H   H  O  214-217                                        166 4-Cl 5-Cl                                                                               Me  Me   H   H  O  204-207                                        167 4-Br 5-Cl                                                                               Me  Me   H   H  O  204-208                                        168 4-CF.sub.3                                                                          4-F Me  Me   H   H  O  203-206                                        169 4-Cl 4-F Me  Me   H   H  O  193-196                                        170 4-Br 4-F Me  Me   H   H  O  194-198                                        171 4-CF.sub.3                                                                          5-Cl                                                                               Me  4-FPh                                                                               H   H  O  219-220                                        172 4-Cl 5-Cl                                                                               Me  4-FPh                                                                               H   H  O  209-211                                        173 4-CF.sub.3                                                                          H   Me  Ph   H   H  O  174-176                                        174 4-Cl H   Me  Ph   H   H  O  165-167                                        175 4-Br H   Me  Ph   H   H  O  165-166                                        176 4-CF.sub.3                                                                          5-Cl                                                                               Me  Et   H   H  O  190-192                                        177 4-CF.sub.3                                                                          5-Cl                                                                               Me  allyl                                                                               H   H  O  150-152                                        178 4-Cl 5-Cl                                                                               Me  allyl                                                                               H   H  O  142-145                                        179 5-CF.sub.3                                                                          5-CF.sub.3                                                                         Me  Me   H   H  O  234-236                                        180 4-OCF.sub.3                                                                         5-CF.sub.3                                                                         Me  Me   H   H  O  196-199                                        181 4-OCF.sub.3                                                                         5-Cl                                                                               Me  allyl                                                                               H   H  O  128-130                                        182 4-Cl H   Me  Me   Me  Me O  155-158                                        183 4-Cl H   Me  Me   Me  H  O  wax                                            184 4-CF.sub.3                                                                          H   Ph  Me   Me  Me O  128-130                                        185 4-CF.sub.3                                                                          H   Me  Me   H   H  S  193-197                                        186 4-Cl H   Me  Me   Me  Me S  192-193                                        __________________________________________________________________________

                  TABLE 5                                                          ______________________________________                                          ##STR13##                                                                     CMPD   R.sub.1  R.sub.2 R.sub.3                                                                             R.sub.4                                                                            syn/anti                                                                               m.p. °C.                       ______________________________________                                         187    4-CF.sub.3                                                                              H       Me   H   syn     179-180                               188    4-CF.sub.3                                                                              H       Me   H   anti    212-213                               189    4-CF.sub.3                                                                              5-Cl    Me   H   syn     196-198                               190    4-CF.sub.3                                                                              5-Cl    Me   H   anti    205-207                               191    4-Br     H       Me   H   mix     193-196                               192    4-Br     5-Cl    Me   H   mix     195-200                               193    4-CF.sub.3                                                                              H       i-Pr H   syn     201-202                               194    4-CF.sub.3                                                                              H       i-Pr H   anti    181-183                               195    4-Cl     H       i-Pr H   syn     151-153                               196    4-Cl     H       i-Pr H   mix     203-205                               197    4-Br     H       i-Pr H   mix     200-205                               198    4-CF.sub.3                                                                              5-Cl    i-Pr H   syn     195-196                               199    4-Br     5-Cl    i-Pr H   mix     197-199                               200    4-Cl     5-Cl    i-Pr H   anti    192-196                               201    4-CF.sub.3                                                                              5-Cl    i-Pr H   mix     196-200                               ______________________________________                                    

                  TABLE 6                                                          ______________________________________                                          ##STR14##                                                                     CMPD   R.sub.1  R.sub.2                                                                               R.sub.3                                                                               R.sub.4                                                                            R.sub.5                                                                             R.sub.6                                                                            m.p. °C.                     ______________________________________                                         202    4-CF.sub.3                                                                              5-F    4-FPh  H   H    H   192-194                             203    4-CF.sub.3                                                                              5-F    Ph     H   H    H   154-156                             204    4-Cl     5-F    4-FPh  H   H    H   182-184                             205    4-Br     5-Cl   Ph     H   H    H   192-194                             ______________________________________                                    

                  TABLE 7                                                          ______________________________________                                          ##STR15##                                                                     CMPD  R.sub.1  R.sub.2                                                                               R.sub.3                                                                               R.sub.a                                                                               R.sub.b                                                                             m.p. °C.                       ______________________________________                                         206   4-CF.sub.3                                                                              5-F    4-FPh  Me     H    218-220                               207   4-CF.sub.3                                                                              5-Cl   H      i-Pr   H    238-240                               208   4-CF.sub.3                                                                              5-F    H      Me     H    241-243                               209   4-OCF.sub.3                                                                             5-F    H      Me     H    211-213                               210   4-CF.sub.3                                                                              H      H      Me     Me   222-223                               211   4-Cl     H      H      Me     Me   215-216                               212   4-CF.sub.3                                                                              5-F    H      Me     Me   198-201                               213   4-F      5-F    H      Me     Me   201.5-205                             214   4-CF.sub.3                                                                              H      H      Ph     H    248.5-250                             215   4-Cl     H      H      Ph     H    253-254                               216   4-CF.sub.3                                                                              H      H      Ph     Me   207-209                               217   4-Cl     H      H      Ph     Me   203-205                               218   4-CF.sub.3                                                                              H      H      4-ClPh H    243.5-245                             219   4-Cl     H      H      4-ClPh H    242.5-244                             220   4-CF.sub.3                                                                              5-Cl   H      Ph     H    246-248                               221   4-Br     5-Cl   H      Ph     H    256-258                               222   4-CF.sub.3                                                                              5-Cl   H      4-ClPh H    235-238                               223   4-Br     5-Cl   H      4-ClPh H    260-262                               224   4-CF.sub.3                                                                              H      H      4-FPh  H    253-255                               225   4-Cl     H      H      4-FPh  H    249-250                               226   4-F      H      H      4-FPh  H    244-246                               227   4-CF.sub.3                                                                              5-F    H      Ph     H    >250                                  228   4-Cl     5-F    H      Ph     H    >250                                  229   4-CF.sub.3                                                                              4-Cl   H      4-FPh  H    252.5-253                             230   4-Cl     4-Cl   H      4-FPh  H    260-261                               231   4-CF.sub.3                                                                              4-Cl   H      4-FPh  Me   176-179                               232   4-CF.sub.3                                                                              4-F    H      4-FPh  H    242-244                               233   4-Cl     4-F    H      4-FPh  H    248-250                               ______________________________________                                    

                  TABLE 8                                                          ______________________________________                                          ##STR16##                                                                     CMPD  R.sub.1 R.sub.2                                                                               R.sub.3                                                                               R.sub.4                                                                            R.sub.5                                                                             A      m.p. °C.                    ______________________________________                                         234   4-Cl    5-Cl   Ph     H   H    O      180-182                            235   4-Br    5-Cl   Ph     H   H    O      189-191                            236   4-CF.sub.3                                                                             5-Cl   Ph     H   H    O      211-212                            237   4-Cl    5-Cl   4-FPh  H   H    O      171-173                            238   4-Br    5-Cl   4-FPh  H   H    O      187-189                            239   4-CF.sub.3                                                                             5-Cl   4-FPh  H   H    O      180-185                            240   4-CF.sub.3                                                                             5-F    Ph     H   H    O      197-200                            241   4-Br    5-F    4-FPh  H   H    O      glass                              242   4-CF.sub.3                                                                             5-F    4-FPh  H   H    O      glass                              243   4-Cl    5-Cl   4-FPh  H   H    S      216-218                            244   4-Br    5-Cl   4-FPh  H   H    S      219-221                            245   4-CF.sub.3                                                                             5-Cl   4-FPh  H   H    S      >220                               246   4-Cl    5-Cl   Ph     H   H    S      194-196                            247   4-Br    5-Cl   Ph     H   H    S      210-212                            248   4-CF.sub.3                                                                             5-Cl   Ph     H   H    S      205-208                            249   4-Cl    5-Cl   4-ClPh H   H    S      184-186                            250   4-Br    5-Cl   4-ClPh H   H    S      199-201                            251   4-CF.sub.3                                                                             5-Cl   4-ClPh H   H    S      207-210                            252   4-Cl    4-F    4-FPh  H   H    S      216-218                            253   4-Br    4-F    4-FPh  H   H    S      218-220                            254   4-CF.sub.3                                                                             4-F    4-FPh  H   H    S      217-219                            255   4-Cl    4-F    Ph     H   H    S      195-197                            256   4-CF.sub.3                                                                             4-F    Ph     H   H    S      208-210                            257   4-Cl    5-F    4-FPh  H   H    S      209-211                            258   4-Br    5-F    4-FPh  H   H    S      215-217                            259   4-CF.sub.3                                                                             5-F    4-FPh  H   H    S      202-204                            260   4-CF.sub.3                                                                             H      H      H   H    C(Me).sub.2                                                                           206-210                            261   4-Cl    H      H      H   H    C(Me).sub.2                                                                           208-212                            262   4-OMe   H      H      H   H    C(Me).sub. 2                                                                          177-180                            263   4-CF.sub.3                                                                             H      H      H   H    S      230-235                            ______________________________________                                    

                  TABLE 9                                                          ______________________________________                                          ##STR17##                                                                     CMPD  R.sub.1 R.sub.2                                                                               R.sub.3                                                                             R.sub.5                                                                             R.sub.c                                                                             R.sub.d                                                                             A    m.p. °C.                  ______________________________________                                         264   4-CF.sub.3                                                                             5-Cl   H    H    Me   Me   S    151-153                          265   4-CF.sub.3                                                                             5-Cl   H    Me   Me   H    S    >250                             266   4-CF.sub.3                                                                             5-Cl   H    H    H    Me   S    234-235                          267   4-CF.sub.3                                                                             5-Cl   H    H    Me   Me   O    253-255                          ______________________________________                                    

                  TABLE 10                                                         ______________________________________                                          ##STR18##                                                                     CMPD  Q       V      A       R.sub.2                                                                             R.sub.3                                                                             R.sub.4                                                                             m.p. °C.                    ______________________________________                                         268   Q-5     --     CH.sub.2 CH.sub.2                                                                      H    H    H    173-174                            269   Q-6     S      CH.sub.2 CH.sub.2                                                                      H    H    H    248-249                            ______________________________________                                    

                  TABLE 11                                                         ______________________________________                                          ##STR19##                                                                     R.sub.1     R.sub.2  R.sub.4   R.sub.10                                                                              A                                        ______________________________________                                         4-F         4-F      H         H      CH.sub.2                                 4-Cl        4-F      H         H      CH.sub.2                                 4-OCF.sub.3 4-F      H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              4-F      H         H      CH.sub.2                                 3,4-di-Cl   4-F      H         H      CH.sub.2                                 4-CN        4-Cl     H         H      CH.sub.2                                 4-CO.sub.2 Me                                                                              4-Cl     H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     H         H      CH.sub.2                                 4-OCF.sub.3 4-Cl     H         H      CH.sub.2                                 4-F         5-F      H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         H      CH.sub.2                                 4-OCF.sub.2 CF.sub.2 H                                                                     5-F      H         H      CH.sub.2                                 4-NO.sub.2  5-F      H         H      CH.sub.2                                 4-SCF.sub.2 H                                                                              5-F      H         H      CH.sub.2                                 4-CN        5-F      H         H      CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         H      CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         H      CH.sub.2                                 4-F         5-Cl     H         H      CH.sub.2                                 4-Cl        5-Cl     H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         H      CH.sub.2                                 4-NO.sub.2  5-Cl     H         H      CH.sub.2                                 4-SCF.sub.2 H                                                                              5-Cl     H         H      CH.sub.2                                 4-CN        5-Cl     H         H      CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         H      CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         H      CH.sub.2                                 4-Cl        5-Br     H         H      CH.sub.2                                 4-Br        5-Br     H         H      CH.sub.2                                 4-CF.sub.3  5-Br     H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Br     H         H      CH.sub.2                                 4-OCF.sub.3 5-Br     H         H      CH.sub.2                                 4-Cl        5-CN     H         H      CH.sub.2                                 4-Br        5-CN     H         H      CH.sub.2                                 4-CF.sub.3  5-CN     H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-CN     H         H      CH.sub.2                                 4-OCF.sub.3 5-CN     H         H      CH.sub.2                                 4-Cl        5-OMe    H         H      CH.sub.2                                 4-Br        5-OMe    H         H      CH.sub.2                                 4-CF.sub.3  5-CF.sub.3                                                                              H         H      CH.sub.2                                 4-Cl        5-CF.sub.3                                                                              H         H      CH.sub.2                                 4-Br        5-CF.sub.3                                                                              H         H      CH.sub.2                                 4-OCF.sub.3 5-CF.sub.3                                                                              H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-CF.sub.3                                                                              H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-OCF.sub.2 H                                                                           H         H      CH.sub.2                                 4-OCF.sub.3 5-OCF.sub.2 H                                                                           H         H      CH.sub.2                                 4-CF.sub.3  5-OCF.sub.2 H                                                                           H         H      CH.sub.2                                 4-Cl        5-OCF.sub.2 H                                                                           H         H      CH.sub.2                                 4-Br        5-OCF.sub.2 H                                                                           H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-OCF.sub.3                                                                             H         H      CH.sub.2                                 4-OCF.sub.3 5-OCF.sub.3                                                                             H         H      CH.sub.2                                 4-CF.sub.3  5-OCF.sub.3                                                                             H         H      CH.sub.2                                 4-Cl        5-OCF.sub.3                                                                             H         H      CH.sub.2                                 4-Br        5-OCF.sub.3                                                                             H         H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-OPh    H         H      CH.sub.2                                 4-OCF.sub.3 5-OPh    H         H      CH.sub.2                                 4-CF.sub.3  5-OPh    H         H      CH.sub.2                                 4-Cl        5-OPh    H         H      CH.sub.2                                 4-Br        5-OPh    H         H      CH.sub.2                                 4-CF.sub.3  5-SMe    H         H      CH.sub.2                                 4-Cl        5-SMe    H         H      CH.sub.2                                 4-Br        5-SMe    H         H      CH.sub.2                                 4-CF.sub.3  6-F      H         H      CH.sub.2                                 4-Cl        6-F      H         H      CH.sub.2                                 4-Br        6-F      H         H      CH.sub.2                                 4-CF.sub.3  6-Cl     H         H      CH.sub.2                                 4-Cl        6-Cl     H         H      CH.sub.2                                 4-Br        6-Cl     H         H      CH.sub.2                                 4-SCF.sub.2 H                                                                              5-F      H         4-F    CH.sub.2                                 4-F         5-F      H         4-F    CH.sub.2                                 4-CN        5-F      H         4-F    CH.sub.2                                 4-OCF.sub.2 CF.sub.2 H                                                                     5-F      H         4-F    CH.sub.2                                 4-OCF.sub.3 5-F      H         4-F    CH.sub.2                                 3,4-di-Cl   5-F      H         4-F    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         4-F    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         4-Cl   CH.sub.2                                 4-OCF.sub.3 5-F      H         4-Cl   CH.sub.2                                 4-Cl        5-F      H         4-NO.sub.2                                                                            CH.sub.2                                 4-Br        5-F      H         4-NO.sub.2                                                                            CH.sub.2                                 4-CF.sub.3  5-F      H         4-NO.sub.2                                                                            CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         4-NO.sub.2                                                                            CH.sub.2                                 4-OCF.sub.3 5-F      H         4-NO.sub.2                                                                            CH.sub.2                                 4-Cl        5-F      H         4-CN   CH.sub.2                                 4-Br        5-F      H         4-CN   CH.sub.2                                 4-CF.sub.3  5-F      H         4-CN   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         4-CN   CH.sub.2                                 4-OCF.sub.3 5-F      H         4-CN   CH.sub.2                                 4-Cl        5-F      H         4-OMe  CH.sub.2                                 4-Br        5-F      H         4-OMe  CH.sub.2                                 4-CF.sub.3  5-F      H         4-OMe  CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         4-OMe  CH.sub.2                                 4-OCF.sub.3 5-F      H         4-OMe  CH.sub.2                                 4-Cl        5-F      H         4-CF.sub.3                                                                            CH.sub.2                                 4-Br        5-F      H         4-CF.sub.3                                                                            CH.sub.2                                 4-CF.sub.3  5-F      H         4-CF.sub.3                                                                            CH.sub.2                                 4-OCF.sub.3 5-F      H         4-CF.sub.3                                                                            CH.sub. 2                                4-OCF.sub.2 H                                                                              5-F      H         4-CF.sub.3                                                                            CH.sub.2                                 4-CF.sub.3  5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2                                 4-Cl        5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2                                 4-Br        5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2                                 4-OCF.sub.3 5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2                                 4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     H         4-F    CH.sub.2                                 4-F         5-Cl     H         4-F    CH.sub.2                                 4-OCF.sub.3 5-Cl     H         4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-F    CH.sub.2                                 4-NO.sub.2  5-Cl     H         4-F    CH.sub.2                                 3,4-di-Cl   5-Cl     H         4-F    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         4-F    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         4-F    CH.sub.2                                 4-OCF.sub.3 5-Cl     H         4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-Cl   CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         4-Cl   CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         4-Cl   CH.sub.2                                 4-CN        5-Cl     H         4-Cl   CH.sub.2                                 4-F         5-Cl     H         4-Cl   CH.sub.2                                 4-NO.sub.2  5-Cl     H         4-Cl   CH.sub.2                                 H           5-Cl     H         4-Cl   CH.sub.2                                 4-CF.sub.3  5-CF.sub.3                                                                              H         4-F    CH.sub.2                                 4-OCF.sub.3 5-CF.sub.3                                                                              H         4-F    CH.sub.2                                 4-Cl        5-CF.sub.3                                                                              H         4-F    CH.sub. 2                                4-Br        5-CF.sub.3                                                                              H         4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              5-CF.sub.3                                                                              H         4-F    CH.sub.2                                 4-CF.sub.3  5-CF.sub.3                                                                              H         4-Cl   CH.sub.2                                 4-OCF.sub.3 5-CF.sub.3                                                                              H         4-Cl   CH.sub.2                                 4-Cl        5-CF.sub.3                                                                              H         4-Cl   CH.sub.2                                 4-Br        5-CF.sub.3                                                                              H         4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-CF.sub.3                                                                              H         4-Cl   CH.sub.2                                 4-CF.sub.3  5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2                                 4-Cl        5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2                                 4-Br        5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2                                 4-OCF.sub.3 5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2                                 4-CF.sub.3  5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2                                 4-Cl        5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2                                 4-Br        5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2                                 4-OCF.sub.3 5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2                                 4-CF.sub.3  4-F      H         4-F    CH.sub.2                                 4-Cl        4-F      H         4-F    CH.sub.2                                 4-Br        4-F      H         4-F    CH.sub.2                                 4-OCF.sub.3 4-F      H         4-F    CH.sub.2                                 4-CF.sub.3  4-F      H         4-Cl   CH.sub.2                                 4-Cl        4-F      H         4-Cl   CH.sub.2                                 4-Br        4-F      H         4-Cl   CH.sub.2                                 4-CF.sub.3  4-Cl     H         4-Cl   CH.sub.2                                 4-Cl        4-Cl     H         4-Cl   CH.sub.2                                 4-Br        4-Cl     H         4-Cl   CH.sub.2                                 4-OCF.sub.3 4-Cl     H         4-Cl   CH.sub.2                                 4-CF.sub.3  4-Cl     H         4-F    CH.sub.2                                 4-Cl        4-Cl     H         4-F    CH.sub.2                                 4-Br        4-Cl     H         4-F    CH.sub.2                                 4-OCF.sub.3 4-Cl     H         4-F    CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            CH.sub.2                                 4-Cl        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2                                 4-Br        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2                                 4-OCF.sub.3 5-Cl     H         4-CF.sub.3                                                                            CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-SMe  CH.sub.2                                 4-Cl        5-Cl     H         4-SMe  CH.sub.2                                 4-Br        5-Cl     H         4-SMe  CH.sub.2                                 4-OCF.sub.3 5-Cl     H         4-SMe  CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-NO.sub.2                                                                            CH.sub.2                                 4-Cl        5-Cl     H         4-NO.sub.2                                                                            CH.sub.2                                 4-Br        5-Cl     H         4-NO.sub.2                                                                            CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-NO.sub.2                                                                            CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-OMe  CH.sub.2                                 4-Cl        5-Cl     H         4-OMe  CH.sub.2                                 4-Br        5-Cl     H         4-OMe  CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-OMe  CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-OPh  CH.sub.2                                 4-Cl        5-Cl     H         4-OPh  CH.sub.2                                 4-Br        5-Cl     H         4-OPh  CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-OPh  CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-CN   CH.sub.2                                 4-Cl        5-Cl     H         4-CN   CH.sub.2                                 4-Br        5-Cl     H         4-CN   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     H         4-CN   CH.sub.2                                 4-CF.sub.3  5-Cl     H         4-CO.sub.2 Me                                                                         CH.sub.2                                 4-Cl        5-Cl     H         4-CO.sub.2 Me                                                                         CH.sub.2                                 4-Br        5-Cl     H         4-CO.sub.2 Me                                                                         CH.sub.2                                 4-CF.sub.3  H        Me        H      CH.sub.2                                 4-Cl        H        Me        H      CH.sub.2                                 4-Br        H        Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              H        Me        H      CH.sub.2                                 4-OCF.sub.3 H        Me        H      CH.sub.2                                 4-CF.sub.3  4-F      Me        H      CH.sub.2                                 4-Cl        4-F      Me        H      CH.sub.2                                 4-Br        4-F      Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              4-F      Me        H      CH.sub.2                                 4-OCF.sub.3 4-F      Me        H      CH.sub.2                                 4-CF.sub.3  4-Cl     Me        H      CH.sub.2                                 4-Cl        4-Cl     Me        H      CH.sub.2                                 4-Br        4-Cl     Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     Me        H      CH.sub.2                                 4-CF.sub.3  5-F      Me        H      CH.sub.2                                 4-Cl        5-F      Me        H      CH.sub.2                                 4-Br        5-F      Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      Me        H      CH.sub.2                                 4-CF.sub.3  5-Cl     Me        H      CH.sub.2                                 4-Cl        5-Cl     Me        H      CH.sub.2                                 4-Br        5-Cl     Me        H      CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        H      CH.sub.2                                 4-CF.sub.3  4-F      Me        4-F    CH.sub.2                                 4-Cl        4-F      Me        4-F    CH.sub.2                                 4-Br        4-F      Me        4-F    CH.sub.2                                 4-OCF.sub. 2 H                                                                             4-F      Me        4-F    CH.sub.2                                 4-CF.sub.3  4-Cl     Me        4-F    CH.sub.2                                 4-Cl        4-Cl     Me        4-F    CH.sub.2                                 4-Br        4-Cl     Me        4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     Me        4-F    CH.sub.2                                 4-CF.sub.3  5-F      Me        4-F    CH.sub.2                                 4-Cl        5-F      Me        4-F    CH.sub.2                                 4-Br        5-F      Me        4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      Me        4-F    CH.sub.2                                 4-CF.sub.3  5-Cl     Me        4-F    CH.sub.2                                 4-Cl        5-Cl     Me        4-F    CH.sub.2                                 4-Br        5-Cl     Me        4-F    CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        4-F    CH.sub.2                                 4-CF.sub.3  4-F      Me        4-Cl   CH.sub.2                                 4-Cl        4-F      Me        4-Cl   CH.sub.2                                 4-Br        4-F      Me        4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   CH.sub.2                                 4-CF.sub.3  4-Cl     Me        4-Cl   CH.sub.2                                 4-Cl        4-Cl     Me        4-Cl   CH.sub.2                                 4-Br        4-Cl     Me        4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   CH.sub.2                                 4-CF.sub.3  5-F      Me        4-Cl   CH.sub.2                                 4-Cl        5-F      Me        4-Cl   CH.sub.2                                 4-Br        5-F      Me        4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   CH.sub.2                                 4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2                                 4-Cl        5-Cl     Me        4-Cl   CH.sub.2                                 4-Br        5-Cl     Me        4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2                                 4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2                                 4-Cl        5-Cl     Me        4-Cl   CH.sub.2                                 4-Br        5-Cl     Me        4-Cl   CH.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2                                 4-CF.sub.3  5-Cl     Et        4-F    CH.sub.2                                 4-Cl        5-Cl     Et        4-F    CH.sub.2                                 4-Br        5-Cl     Et        4-F    CH.sub.2                                 4-CF.sub.3  5-Cl     Et        4-Cl   CH.sub.2                                 4-Cl        5-Cl     Et        4-Cl   CH.sub.2                                 4-Br        5-Cl     Et        4-Cl   CH.sub.2                                 4-CF.sub.3  5-Cl     allyl     4-F    CH.sub.2                                 4-Cl        5-Cl     allyl     4-F    CH.sub.2                                 4-Br        5-Cl     allyl     4-F    CH.sub.2                                 4-CF.sub.3  5-Cl     allyl     4-Cl   CH.sub.2                                 4-Cl        5-Cl     allyl     4-Cl   CH.sub.2                                 4-Br        5-Cl     allyl     4-Cl   CH.sub.2                                 4-CF.sub.3  5-Cl     propargyl 4-F    CH.sub.2                                 4-Cl        5-Cl     propargyl 4-F    CH.sub.2                                 4-Br        5-Cl     propargyl 4-F    CH.sub.2                                 4-CF.sub.3  5-Cl     propargyl 4-Cl   CH.sub.2                                 4-Cl        5-Cl     propargyl 4-Cl   CH.sub.2                                 4-Br        5-Cl     propargyl 4-Cl   CH.sub.2                                 4-CF.sub.3  5-F      H         4-F    O                                        4-OCF.sub.3 5-F      H         4-F    O                                        4-CF.sub.3  4-F      H         4-F    O                                        4-OCF.sub.3 4-F      H         4-F    O                                        4-CF.sub.3  5-Cl     H         4-F    O                                        4-OCF.sub.3 5-Cl     H         4-F    O                                        4-CF.sub.3  5-CF.sub.3                                                                              H         4-F    O                                        4-OCF.sub.3 5-CF.sub.3                                                                              H         4-F    O                                        4-CF.sub.3  5-F      H         4-F    S                                        4-OCF.sub.3 5-F      H         4-F    S                                        4-CF.sub. 3 4-F      H         4-F    S                                        4-OCF.sub.3 4-F      H         4-F    S                                        4-CF.sub.3  5-Cl     H         4-F    S                                        4-OCF.sub.3 5-Cl     H         4-F    S                                        4-CF.sub.3  5-CF.sub.3                                                                              H         4-F    S                                        4-OCF.sub.3 5-CF.sub.3                                                                              H         4-F    S                                        4-CF.sub.3  H        Me        H      O                                        4-Cl        H        Me        H      O                                        4-Br        H        Me        H      O                                        4-OCF.sub.2 H                                                                              H        Me        H      O                                        4-OCF.sub.3 H        Me        H      O                                        4-CF.sub.3  4-F      Me        H      O                                        4-Cl        4-F      Me        H      O                                        4-Br        4-F      Me        H      O                                        4-OCF.sub.2 H                                                                              4-F      Me        H      O                                        4-OCF.sub.3 4-F      Me        H      O                                        4-CF.sub.3  4-Cl     Me        H      O                                        4-Cl        4-Cl     Me        H      O                                        4-Br        4-Cl     Me        H      O                                        4-OCF.sub.2 H                                                                              4-Cl     Me        H      O                                        4-OCF.sub.3 4-Cl     Me        H      O                                        4-CF.sub.3  5-F      Me        H      O                                        4-Cl        5-F      Me        H      O                                        4-Br        5-F      Me        H      O                                        4-OCF.sub.2 H                                                                              5-F      Me        H      O                                        4-CF.sub.3  5-Cl     Me        H      O                                        4-Cl        5-Cl     Me        H      O                                        4-Br        5-Cl     Me        H      O                                        4-OCF.sub.3 5-Cl     Me        H      O                                        4-OCF.sub.2 H                                                                              5-Cl     Me        H      O                                        4-CF.sub.3  4-F      Me        4-F    O                                        4-Cl        4-F      Me        4-F    O                                        4-Br        4-F      Me        4-F    O                                        4-OCF.sub.3 4-F      Me        4-F    O                                        4-OCF.sub.2 H                                                                              4-F      Me        4-F    O                                        4-CF.sub.3  4-Cl     Me        4-F    O                                        4-Cl        4-Cl     Me        4-F    O                                        4-Br        4-Cl     Me        4-F    O                                        4-OCF.sub.3 4-Cl     Me        4-F    O                                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-F    O                                        4-CF.sub.3  5-F      Me        4-F    O                                        4-Cl        5-F      Me        4-F    O                                        4-Br        5-F      Me        4-F    O                                        4-OCF.sub.3 5-F      Me        4-F    O                                        4-OCF.sub.2 H                                                                              5-F      Me        4-F    O                                        4-CF.sub.3  5-Cl     Me        4-F    O                                        4-Cl        5-Cl     Me        4-F    O                                        4-Br        5-Cl     Me        4-F    O                                        4-OCF.sub.3 5-Cl     Me        4-F    O                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-F    O                                        4-CF.sub.3  4-F      Me        4-Cl   O                                        4-Cl        4-F      Me        4-Cl   O                                        4-Br        4-F      Me        4-Cl   O                                        4-OCF.sub.3 4-F      Me        4-Cl   O                                        4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   O                                        4-CF.sub.3  4-Cl     Me        4-Cl   O                                        4-Cl        4-Cl     Me        4-Cl   O                                        4-Br        4-Cl     Me        4-Cl   O                                        4-OCF.sub.3 4-Cl     Me        4-Cl   O                                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   O                                        4-CF.sub.3  5-F      Me        4-Cl   O                                        4-Cl        5-F      Me        4-Cl   O                                        4-Br        5-F      Me        4-Cl   O                                        4-OCF.sub.3 5-F      Me        4-Cl   O                                        4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   O                                        4-CF.sub.3  5-Cl     Me        4-Cl   O                                        4-Cl        5-Cl     Me        4-Cl   O                                        4-Br        5-Cl     Me        4-Cl   O                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   O                                        4-OCF.sub.3 5-Cl     Me        4-Cl   O                                        4-CF.sub.3  5-Cl     Me        4-Cl   O                                        4-Cl        5-Cl     Me        4-Cl   O                                        4-Br        5-Cl     Me        4-Cl   O                                        4-OCF.sub.3 5-Cl     Me        4-Cl   O                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   O                                        4-CF.sub.3  5-Cl     Et        4-F    O                                        4-Cl        5-Cl     Et        4-F    O                                        4-Br        5-Cl     Et        4-F    O                                        4-CF.sub.3  5-Cl     Et        4-Cl   O                                        4-Cl        5-Cl     Et        4-Cl   O                                        4-Br        5-Cl     Et        4-Cl   O                                        4-CF.sub.3  5-Cl     allyl     4-F    O                                        4-Cl        5-Cl     allyl     4-F    O                                        4-Br        5-Cl     allyl     4-F    O                                        4-CF.sub.3  5-Cl     allyl     4-Cl   O                                        4-Cl        5-Cl     allyl     4-Cl   O                                        4-Br        5-Cl     allyl     4-Cl   O                                        4-CF.sub.3  5-Cl     propargyl 4-F    O                                        4-Cl        5-Cl     propargyl 4-F    O                                        4-Br        5-Cl     propargyl 4-F    O                                        4-CF.sub.3  5-Cl     propargyl 4-Cl   O                                        4-Cl        5-Cl     propargyl 4-Cl   O                                        4-Br        5-Cl     propargyl 4-Cl   O                                        4-CF.sub.3  H        Me        H      S                                        4-Cl        H        Me        H      S                                        4-Br        H        Me        H      S                                        4-OCF.sub.2 H                                                                              H        Me        H      S                                        4-OCF.sub.3 H        Me        H      S                                        4-CF.sub.3  4-F      Me        H      S                                        4-Cl        4-F      Me        H      S                                        4-Br        4-F      Me        H      S                                        4-OCF.sub.2 H                                                                              4-F      Me        H      S                                        4-OCF.sub.3 4-F      Me        H      S                                        4-CF.sub.3  4-Cl     Me        H      S                                        4-Cl        4-Cl     Me        H      S                                        4-Br        4-Cl     Me        H      S                                        4-OCF.sub.2 H                                                                              4-Cl     Me        H      S                                        4-OCF.sub.3 4-Cl     Me        H      S                                        4-CF.sub.3  5-F      Me        H      S                                        4-Cl        5-F      Me        H      S                                        4-Br        5-F      Me        H      S                                        4-OCF.sub.2 H                                                                              5-F      Me        H      S                                        4-CF.sub.3  5-Cl     Me        H      S                                        4-Cl        5-Cl     Me        H      S                                        4-Br        5-Cl     Me        H      S                                        4-OCF.sub.2 H                                                                              5-Cl     Me        H      S                                        4-CF.sub.3  4-F      Me        4-F    S                                        4-Cl        4-F      Me        4-F    S                                        4-Br        4-F      Me        4-F    S                                        4-OCF.sub.2 H                                                                              4-F      Me        4-F    S                                        4-CF.sub.3  4-Cl     Me        4-F    S                                        4-Cl        4-Cl     Me        4-F    S                                        4-Br        4-Cl     Me        4-F    S                                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-F    S                                        4-CF.sub.3  5-F      Me        4-F    S                                        4-Cl        5-F      Me        4-F    S                                        4-Br        5-F      Me        4-F    S                                        4-OCF.sub.2 H                                                                              5-F      Me        4-F    S                                        4-CF.sub.3  5-Cl     Me        4-F    S                                        4-Cl        5-Cl     Me        4-F    S                                        4-Br        5-Cl     Me        4-F    S                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-F    S                                        4-CF.sub.3  4-F      Me        4-Cl   S                                        4-Cl        4-F      Me        4-Cl   S                                        4-Br        4-F      Me        4-Cl   S                                        4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   S                                        4-CF.sub.3  4-Cl     Me        4-Cl   S                                        4-Cl        4-Cl     Me        4-Cl   S                                        4-Br        4-Cl     Me        4-Cl   S                                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   S                                        4-CF.sub.3  5-F      Me        4-Cl   S                                        4-Cl        5-F      Me        4-Cl   S                                        4-Br        5-F      Me        4-Cl   S                                        4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   S                                        4-CF.sub.3  5-Cl     Me        4-Cl   S                                        4-Cl        5-Cl     Me        4-Cl   S                                        4-Br        5-Cl     Me        4-Cl   S                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   S                                        4-CF.sub.3  5-Cl     Me        4-Cl   S                                        4-Cl        5-Cl     Me        4-Cl   S                                        4-Br        5-Cl     Me        4-Cl   S                                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   S                                        4-CF.sub.3  5-Cl     Et        4-F    S                                        4-Cl        5-Cl     Et        4-F    S                                        4-Br        5-Cl     Et        4-F    S                                        4-CF.sub.3  5-Cl     Et        4-Cl   S                                        4-Cl        5-Cl     Et        4-Cl   S                                        4-Br        5-Cl     Et        4-Cl   S                                        4-CF.sub.3  5-Cl     allyl     4-F    S                                        4-Cl        5-Cl     allyl     4-F    S                                        4-Br        5-Cl     allyl     4-F    S                                        4-CF.sub.3  5-Cl     allyl     4-Cl   S                                        4-Cl        5-Cl     allyl     4-Cl   S                                        4-Br        5-Cl     allyl     4-Cl   S                                        4-CF.sub.3  5-Cl     propargyl 4-F    S                                        4-Cl        5-Cl     propargyl 4-F    S                                        4-Br        5-Cl     propargyl 4-F    S                                        4-CF.sub.3  5-Cl     propargyl 4-Cl   S                                        4-Cl        5-Cl     propargyl 4-Cl   S                                        4-Br        5-Cl     propargyl 4-Cl   S                                        4-Cl        H        H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 H        H         H      CH.sub.2 CH.sub.2                        4-F         4-F      H         H      CH.sub.2 CH.sub.2                        4-Cl        4-F      H         H      CH.sub.2 CH.sub.2                        4-Br        4-F      H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 4-F      H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-F      H         H      CH.sub.2 CH.sub.2                        3,4-di-Cl   4-F      H         H      CH.sub.2 CH.sub.2                        4-CN        4-Cl     H         H      CH.sub.2 CH.sub.2                        4-CO.sub.2 Me                                                                              4-Cl     H         H      CH.sub.2 CH.sub.2                        4-Cl        4-Cl     H         H      CH.sub.2 CH.sub.2                        4-Br        4-Cl     H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-Cl     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 4-Cl     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         H      CH.sub.2 CH.sub.2                        4-NO.sub.2  5-F      H         H      CH.sub.2 CH.sub.2                        4-SCF.sub.2 H                                                                              5-F      H         H      CH.sub.2 CH.sub.2                        4-CN        5-F      H         H      CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         H      CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         H      CH.sub.2 CH.sub.2                        4-F         5-Cl     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-Cl     H         H      CH.sub.2 CH.sub.2                        4-NO.sub.2  5-Cl     H         H      CH.sub.2 CH.sub.2                        4-SCF.sub.2 H                                                                              5-Cl     H         H      CH.sub.2 CH.sub.2                        4-CN        5-Cl     H         H      CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         H      CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         H      CH.sub.2 CH.sub.2                        4-Cl        5-Br     H         H      CH.sub.2 CH.sub.2                        4-Br        5-Br     H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Br     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Br     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-Br     H         H      CH.sub.2 CH.sub.2                        4-Cl        5-CN     H         H      CH.sub.2 CH.sub.2                        4-Br        5-CN     H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-CN     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-CN     H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-CN     H         H      CH.sub.2 CH.sub.2                        4-Cl        5-OMe    H         H      CH.sub.2 CH.sub.2                        4-Br        5-OMe    H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OMe    H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-OCF.sub.2 H                                                                           H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-OCF.sub.2 H                                                                           H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OCF.sub.2 H                                                                           H         H      CH.sub. 2 CH.sub.2                       4-Cl        5-OCF.sub.2 H                                                                           H         H      CH.sub.2 CH.sub.2                        4-Br        5-OCF.sub.2 H                                                                           H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-OCF.sub.3                                                                             H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-OCF.sub.3                                                                             H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OCF.sub.3                                                                             H         H      CH.sub.2 CH.sub.2                        4-Cl        5-OCF.sub.3                                                                             H         H      CH.sub.2 CH.sub.2                        4-Br        5-OCF.sub.3                                                                             H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-OPh    H         H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-OPh    H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OPh    H         H      CH.sub.2 CH.sub.2                        4-Cl        5-OPh    H         H      CH.sub.2 CH.sub.2                        4-Br        5-OPh    H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-SMe    H         H      CH.sub.2 CH.sub.2                        4-Cl        5-SMe    H         H      CH.sub.2 CH.sub.2                        4-Br        5-SMe    H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  6-F      H         H      CH.sub.2 CH.sub.2                        4-Cl        6-F      H         H      CH.sub.2 CH.sub.2                        4-Br        6-F      H         H      CH.sub.2 CH.sub.2                        4-CF.sub.3  6-Cl     H         H      CH.sub.2 CH.sub.2                        4-Cl        6-Cl     H         H      CH.sub.2 CH.sub.2                        4-Br        6-Cl     H         H      CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-F    CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         4-F    CH.sub.2 CH.sub.2                        3,4-di-Cl   5-F      H         4-F    CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         4-F    CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         4-F    CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-CN   CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-CN   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-CN   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-CN   CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         4-CN   CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2 CH.sub.2                        4-Cl        5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2 CH.sub.2                        4-Br        5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-F      H         4-OCF.sub.2 H                                                                         CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-F         5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-NO.sub.2  5-Cl     H         4-F    CH.sub.2 CH.sub.2                        3,4-di-Cl   5-Cl     H         4-F    CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         4-F    CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-CN        5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-F         5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-NO.sub.2  5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        H           5-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-CF.sub.3                                                                              H         4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-CF.sub.3                                                                              H         4-F    CH.sub.2 CH.sub.2                        4-Cl        5-CF.sub.3                                                                              H         4-F    CH.sub.2 CH.sub.2                        4-Br        5-CF.sub.3                                                                              H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2 CH.sub.2                        4-Cl        5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2 CH.sub.2                        4-Br        5-OCF.sub.2 H                                                                           H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-OCF.sub.2 H                                                                           H         4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      H         4-F    CH.sub.2 CH.sub.2                        4-Cl        4-F      H         4-F    CH.sub.2 CH.sub.2                        4-Br        4-F      H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-Cl        4-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-Br        4-F      H         4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-Cl        4-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-Br        4-Cl     H         4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-Cl        4-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-Br        4-Cl     H         4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-Me   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-Me   CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-Me   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-Me   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-SMe  CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-SMe  CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-SMe  CH.sub.2 CH.sub.2                        4-OCF.sub.3 5-Cl     H         4-SMe  CH.sub.2 CH.sub.2                        4-CF.sub. 3 5-Cl     H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-NO.sub.2                                                                            CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     H         4-OPh  CH.sub.2 CH.sub.2                        4-Cl        5-Cl     H         4-OPh  CH.sub.2 CH.sub.2                        4-Br        5-Cl     H         4-OPh  CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     H         4-OPh  CH.sub.2 CH.sub.2                        4-CF.sub.3  H        Me        H      CH.sub.2 CH.sub.2                        4-Cl        H        Me        H      CH.sub.2 CH.sub.2                        4-Br        H        Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              H        Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 H        Me        H      CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      Me        H      CH.sub.2 CH.sub.2                        4-Cl        4-F      Me        H      CH.sub.2 CH.sub.2                        4-Br        4-F      Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-F      Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 4-F      Me        H      CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     Me        H      CH.sub.2 CH.sub.2                        4-Cl        4-Cl     Me        H      CH.sub.2 CH.sub.2                        4-Br        4-Cl     Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-Cl     Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.3 4-Cl     Me        H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      Me        H      CH.sub.2 CH.sub.2                        4-Cl        5-F      Me        H      CH.sub.2 CH.sub.2                        4-Br        5-F      Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      Me        H      CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Me        H      CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Me        H      CH.sub.2 CH.sub.2                        4-Br        5-Cl     Me        H      CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     Me        H      CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      Me        4-F    CH.sub.2 CH.sub.2                        4-Cl        4-F      Me        4-F    CH.sub.2 CH.sub.2                        4-Br        4-F      Me        4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-F      Me        4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-Cl        4-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-Br        4-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      Me        4-F    CH.sub.2 CH.sub.2                        4-Cl        5-F      Me        4-F    CH.sub.2 CH.sub.2                        4-Br        5-F      Me        4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      Me        4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-Br        5-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  4-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        4-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-Br        4-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  4-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        4-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Br        4-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Et        4-F    CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Et        4-F    CH.sub.2 CH.sub.2                        4-Br        5-Cl     Et        4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     Et        4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     Et        4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     Et        4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     allyl     4-F    CH.sub.2 CH.sub.2                        4-Cl        5-Cl     allyl     4-F    CH.sub.2 CH.sub.2                        4-Br        5-Cl     allyl     4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     allyl     4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     allyl     4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     allyl     4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     propargyl 4-F    CH.sub.2 CH.sub.2                        4-Cl        5-Cl     propargyl 4-F    CH.sub.2 CH.sub.2                        4-Br        5-Cl     propargyl 4-F    CH.sub.2 CH.sub.2                        4-CF.sub.3  5-Cl     propargyl 4-Cl   CH.sub.2 CH.sub.2                        4-Cl        5-Cl     propargyl 4-Cl   CH.sub.2 CH.sub.2                        4-Br        5-Cl     propargyl 4-Cl   CH.sub.2 CH.sub.2                        4-CF.sub.3  5-F      H         4-F    NMe                                      4-OCF.sub.3 5-F      H         4-F    NMe                                      4-CF.sub.3  5-Cl     H         4-F    NMe                                      4-OCF.sub.3 5-Cl     H         4-F    NMe                                      4-CF.sub.3  4-F      Me        4-Cl   NMe                                      4-Cl        4-F      Me        4-Cl   NMe                                      4-Br        4-F      Me        4-Cl   NMe                                      4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   NMe                                      4-CF.sub.3  4-Cl     Me        4-Cl   NMe                                      4-Cl        4-Cl     Me        4-Cl   NMe                                      4-Br        4-Cl     Me        4-Cl   NMe                                      4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   NMe                                      4-CF.sub.3  5-F      Me        4-Cl   NMe                                      4-Cl        5-F      Me        4-Cl   NMe                                      4-Br        5-F      Me        4-Cl   NMe                                      4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   NMe                                      4-CF.sub.3  5-Cl     Me        4-Cl   NMe                                      4-Cl        5-Cl     Me        4-Cl   NMe                                      4-Br        5-Cl     Me        4-Cl   NMe                                      4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   NMe                                      4-CF.sub.3  5-Cl     Me        4-Cl   NMe                                      4-Cl        5-Cl     Me        4-Cl   NMe                                      4-Br        5-Cl     Me        4-Cl   NMe                                      4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   NMe                                      4-F         5-F      H         H      CHMe                                     4-Cl        5-F      H         H      CHMe                                     4-Br        5-F      H         H      CHMe                                     4-CF.sub.3  5-F      H         H      CHMe                                     4-OCF.sub.2 H                                                                              5-F      H         H      CHMe                                     4-OCF.sub.3 5-F      H         H      CHMe                                     4-NO.sub.2  5-F      H         H      CHMe                                     4-SCF.sub.2 H                                                                              5-F      H         H      CHMe                                     4-CN        5-F      H         H      CHMe                                     3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         H      CHMe                                     3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         H      CHMe                                     4-F         5-Cl     H         H      CHMe                                     4-Cl        5-Cl     H         H      CHMe                                     4-Br        5-Cl     H         H      CHMe                                     4-CF.sub.3  5-Cl     H         H      CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     H         H      CHMe                                     4-OCF.sub.3 5-Cl     H         H      CHMe                                     4-NO.sub.2  5-Cl     H         H      CHMe                                     4-CF.sub.3  4-Cl     H         4-Cl   CHMe                                     4-Cl        4-Cl     H         4-Cl   CHMe                                     4-Br        4-Cl     H         4-Cl   CHMe                                     4-CF.sub.3  4-Cl     H         4-F    CHMe                                     4-Cl        4-Cl     H         4-F    CHMe                                     4-Br        4-Cl     H         4-F    CHMe                                     4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            CHMe                                     4-Cl        5-Cl     H         4-CF.sub.3                                                                            CHMe                                     4-Br        5-Cl     H         4-CF.sub.3                                                                            CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            CHMe                                     4-CF.sub.3  5-Cl     H         4-Me   CHMe                                     4-Cl        5-Cl     H         4-Me   CHMe                                     4-Br        5-Cl     H         4-Me   CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     H         4-Me   CHMe                                     4-CF.sub.3  5-Cl     H         4-SMe  CHMe                                     4-Cl        5-Cl     H         4-SMe  CHMe                                     4-Br        5-Cl     H         4-SMe  CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     H         4-SMe  CHMe                                     4-CF.sub.3  4-F      Me        4-Cl   CHMe                                     4-Cl        4-F      Me        4-Cl   CHMe                                     4-Br        4-F      Me        4-Cl   CHMe                                     4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   CHMe                                     4-CF.sub.3  4-Cl     Me        4-Cl   CHMe                                     4-Cl        4-Cl     Me        4-Cl   CHMe                                     4-Br        4-Cl     Me        4-Cl   CHMe                                     4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   CHMe                                     4-CF.sub.3  5-F      Me        4-Cl   CHMe                                     4-Cl        5-F      Me        4-Cl   CHMe                                     4-Br        5-F      Me        4-Cl   CHMe                                     4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   CHMe                                     4-CF.sub.3  5-Cl     Me        4-Cl   CHMe                                     4-Cl        5-Cl     Me        4-Cl   CHMe                                     4-Br        5-Cl     Me        4-Cl   CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CHMe                                     4-CF.sub.3  5-Cl     Me        4-Cl   CHMe                                     4-Cl        5-Cl     Me        4-Cl   CHMe                                     4-Br        5-Cl     Me        4-Cl   CHMe                                     4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CHMe                                     4-CF.sub.3  4-F      Me        4-Cl   SO.sub.2                                 4-Cl        4-F      Me        4-Cl   SO.sub.2                                 4-Br        4-F      Me        4-Cl   SO.sub.2                                 4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   SO.sub.2                                 4-CF.sub.3  4-Cl     Me        4-Cl   SO.sub.2                                 4-Cl        4-Cl     Me        4-Cl   SO.sub.2                                 4-Br        4-Cl     Me        4-Cl   SO.sub.2                                 4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   SO.sub.2                                 4-CF.sub.3  5-F      Me        4-Cl   SO.sub.2                                 4-Cl        5-F      Me        4-Cl   SO.sub.2                                 4-Br        5-F      Me        4-Cl   SO.sub.2                                 4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   SO.sub.2                                 4-CF.sub.3  5-Cl     Me        4-Cl   SO.sub.2                                 4-Cl        5-Cl     Me        4-Cl   SO.sub.2                                 4-Br        5-Cl     Me        4-Cl   SO.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   SO.sub.2                                 4-CF.sub.3  5-Cl     Me        4-Cl   SO.sub.2                                 4-Cl        5-Cl     Me        4-Cl   SO.sub.2                                 4-Br        5-Cl     Me        4-Cl   SO.sub.2                                 4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   SO.sub.2                                 4-F         5-F      H         H      C(Me).sub.2                              4-Cl        5-F      H         H      C(Me).sub.2                              4-Br        5-F      H         H      C(Me).sub.2                              4-CF.sub.3  5-F      H         H      C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-F      H         H      C(Me).sub.2                              4-OCF.sub.3 5-F      H         H      C(Me).sub.2                              4-NO.sub.2  5-F      H         H      C(Me).sub.2                              4-SCF.sub.2 H                                                                              5-F      H         H      C(Me).sub.2                              4-CN        5-F      H         H      C(Me).sub.2                              3,4-CF.sub.2 CF.sub.2 O                                                                    5-F      H         H      C(Me).sub.2                              3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         H      C(Me).sub.2                              4-F         5-Cl     H         H      C(Me).sub.2                              4-Cl        5-Cl     H         H      C(Me).sub.2                              4-Br        5-Cl     H         H      C(Me).sub.2                              4-CF.sub.3  5-Cl     H         H      C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     H         H      C(Me).sub.2                              4-OCF.sub.3 5-Cl     H         H      C(Me).sub.2                              4-NO.sub.2  5-Cl     H         H      C(Me).sub.2                              4-CF.sub.3  4-Cl     H         4-Cl   C(Me).sub.2                              4-Cl        4-Cl     H         4-Cl   C(Me).sub.2                              4-Br        4-Cl     H         4-Cl   C(Me).sub.2                              4-CF.sub.3  4-Cl     H         4-F    C(Me).sub.2                              4-Cl        4-Cl     H         4-F    C(Me).sub.2                              4-Br        4-Cl     H         4-F    C(Me).sub.2                              4-OCF.sub.3 4-Cl     H         4-F    C(Me).sub.2                              4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            C(Me).sub.2                              4-Cl        5-Cl     H         4-CF.sub.3                                                                            C(Me).sub.2                              4-Br        5-Cl     H         4-CF.sub.3                                                                            C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            C(Me).sub.2                              4-OCF.sub.3 5-Cl     H         4-CF.sub.3                                                                            C(Me).sub.2                              4-CF.sub.3  5-Cl     H         4-Me   C(Me).sub.2                              4-Cl        5-Cl     H         4-Me   C(Me).sub.2                              4-Br        5-Cl     H         4-Me   C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     H         4-Me   C(Me).sub.2                              4-CF.sub.3  5-F      Me        4-F    C(Me).sub.2                              4-Cl        5-F      Me        4-F    C(Me).sub.2                              4-Br        5-F      Me        4-F    C(Me).sub.2                              4-OCF.sub.3 5-F      Me        4-F    C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-F      Me        4-F    C(Me).sub.2                              4-CF.sub.3  5-Cl     H         4-SMe  C(Me).sub.2                              4-Cl        5-Cl     H         4-SMe  C(Me).sub.2                              4-Br        5-Cl     H         4-SMe  C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     H         4-SMe  C(Me).sub.2                              4-CF.sub.3  4-F      Me        4-Cl   C(Me).sub.2                              4-Cl        4-F      Me        4-Cl   C(Me).sub.2                              4-Br        4-F      Me        4-Cl   C(Me).sub.2                              4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   C(Me).sub.2                              4-CF.sub.3  4-Cl     Me        4-Cl   C(Me).sub.2                              4-Cl        4-Cl     Me        4-Cl   C(Me).sub.2                              4-Br        4-Cl     Me        4-Cl   C(Me).sub.2                              4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   C(Me).sub.2                              4-CF.sub.3  5-F      Me        4-Cl   C(Me).sub.2                              4-Cl        5-F      Me        4-Cl   C(Me).sub.2                              4-Br        5-F      Me        4-Cl   C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   C(Me).sub.2                              4-CF.sub.3  5-Cl     Me        4-Cl   C(Me).sub.2                              4-Cl        5-Cl     Me        4-Cl   C(Me).sub.2                              4-Br        5-Cl     Me        4-Cl   C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   C(Me).sub.2                              4-CF.sub.3  5-Cl     Me        4-Cl   C(Me).sub.2                              4-Cl        5-Cl     Me        4-Cl   C(Me).sub.2                              4-Br        5-Cl     Me        4-Cl   C(Me).sub.2                              4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   C(Me).sub.2                              4-CF.sub.3  5-F      Me        4-F    C(Me).sub.2                              4-OCF.sub.3 5-F      Me        4-F    C(Me).sub.2                              4-CF.sub.3  4-Cl     Me        4-Cl   S(O)                                     4-Cl        4-Cl     Me        4-Cl   S(O)                                     4-Br        4-Cl     Me        4-Cl   S(O)                                     4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   S(O)                                     4-CF.sub.3  5-F      Me        4-Cl   S(O)                                     4-Cl        5-F      Me        4-Cl   S(O)                                     4-Br        5-F      Me        4-Cl   S(O)                                     4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   S(O)                                     4-CF.sub.3  5-Cl     Me        4-Cl   S(O)                                     4-Cl        5-Cl     Me        4-Cl   S(O)                                     4-Br        5-Cl     Me        4-Cl   S(O)                                     4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   S(O)                                     4-CF.sub.3  5-Cl     Me        4-Cl   S(O)                                     4-Cl        5-Cl     Me        4-Cl   S(O)                                     4-Br        5-Cl     Me        4-Cl   S(O)                                     4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   S(O)                                     4-F         5-F      H         H      OCH.sub.2                                4-Cl        5-F      H         H      OCH.sub.2                                4-Br        5-F      H         H      OCH.sub.2                                4-CF.sub.3  5-F      H         H      OCH.sub.2                                4-OCF.sub.2 H                                                                              5-F      H         H      OCH.sub.2                                4-OCF.sub.3 5-F      H         H      OCH.sub.2                                4-CF.sub.3  4-Cl     H         4-Cl   OCH.sub.2                                4-Cl        4-Cl     H         4-Cl   OCH.sub.2                                4-Br        4-Cl     H         4-Cl   OCH.sub.2                                4-CF.sub.3  4-Cl     H         4-F    OCH.sub.2                                4-Cl        4-Cl     H         4-F    OCH.sub.2                                4-Br        4-Cl     H         4-F    OCH.sub.2                                4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            OCH.sub.2                                4-Cl        5-Cl     H         4-CF.sub.3                                                                            OCH.sub.2                                4-Br        5-Cl     H         4-CF.sub.3                                                                            OCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            OCH.sub.2                                4-CF.sub.3  4-F      Me        4-Cl   OCH.sub. 2                               4-Cl        4-F      Me        4-Cl   OCH.sub.2                                4-Br        4-F      Me        4-Cl   OCH.sub.2                                4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   OCH.sub.2                                4-CF.sub.3  4-Cl     Me        4-Cl   OCH.sub.2                                4-Cl        4-Cl     Me        4-Cl   OCH.sub.2                                4-Br        4-Cl     Me        4-Cl   OCH.sub.2                                4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   OCH.sub.2                                4-CF.sub.3  5-F      Me        4-Cl   OCH.sub.2                                4-Cl        5-F      Me        4-Cl   OCH.sub.2                                4-Br        5-F      Me        4-Cl   OCH.sub.2                                4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   OCH.sub.2                                4-CF.sub.3  5-Cl     Me        4-Cl   OCH.sub.2                                4-Cl        5-Cl     Me        4-Cl   OCH.sub.2                                4-Br        5-Cl     Me        4-Cl   OCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   OCH.sub.2                                4-CF.sub.3  5-Cl     Me        4-Cl   OCH.sub.2                                4-Cl        5-Cl     Me        4-Cl   OCH.sub.2                                4-Br        5-Cl     Me        4-Cl   OCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   OCH.sub.2                                4-F         5-F      H         H      CH.sub.2 O                               4-Cl        5-F      H         H      CH.sub.2 O                               4-Br        5-F      H         H      CH.sub.2 O                               4-CF.sub.3  5-F      H         H      CH.sub.2 O                               4-OCF.sub.2 H                                                                              5-F      H         H      CH.sub.2 O                               4-OCF.sub.3 5-F      H         H      CH.sub.2 O                               4-NO.sub.2  5-F      H         H      CH.sub.2 O                               4-SCF.sub.2 H                                                                              5-F      H         H      CH.sub.2 O                               4-CN        5-F      H         H      CH.sub.2 O                               3,4-CF.sub. 2 CF.sub.2 O                                                                   5-F      H         H      CH.sub.2 O                               3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-F      H         H      CH.sub.2 O                               4-CF.sub.3  4-Cl     H         4-Cl   CH.sub.2 O                               4-Cl        4-Cl     H         4-Cl   CH.sub.2 O                               4-Br        4-Cl     H         4-Cl   CH.sub.2 O                               4-CF.sub.3  4-Cl     H         4-F    CH.sub.2 O                               4-Cl        4-Cl     H         4-F    CH.sub.2 O                               4-Br        4-Cl     H         4-F    CH.sub.2 O                               4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 O                               4-Cl        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 O                               4-Br        5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 O                               4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            CH.sub.2 O                               4-CF.sub.3  4-F      Me        4-Cl   CH.sub.2 O                               4-Cl        4-F      Me        4-Cl   CH.sub.2 O                               4-Br        4-F      Me        4-Cl   CH.sub.2 O                               4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   CH.sub.2 O                               4-CF.sub.3  4-Cl     Me        4-Cl   CH.sub.2 O                               4-Cl        4-Cl     Me        4-Cl   CH.sub.2 O                               4-Br        4-Cl     Me        4-Cl   CH.sub.2 O                               4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   CH.sub.2 O                               4-CF.sub.3  5-F      Me        4-Cl   CH.sub.2 O                               4-Cl        5-F      Me        4-Cl   CH.sub.2 O                               4-Br        5-F      Me        4-Cl   CH.sub.2 O                               4-OCF.sub.2 H                                                                              5-F      Me        4-Cl   CH.sub.2 O                               4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2 O                               4-Cl        5-Cl     Me        4-Cl   CH.sub.2 O                               4-Br        5-Cl     Me        4-Cl   CH.sub.2 O                               4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2 O                               4-CF.sub.3  5-Cl     Me        4-Cl   CH.sub.2 O                               4-Cl        5-Cl     Me        4-Cl   CH.sub.2 O                               4-Br        5-Cl     Me        4-Cl   CH.sub.2 O                               4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   CH.sub.2 O                               4-F         5-F      H         H      SCH.sub.2                                4-Cl        5-F      H         H      SCH.sub.2                                4-Br        5-F      H         H      SCH.sub.2                                4-CF.sub.3  5-F      H         H      SCH.sub.2                                4-OCF.sub.2 H                                                                              5-F      H         H      SCH.sub.2                                4-OCF.sub.3 5-F      H         H      SCH.sub.2                                4-Cl        5-Cl     H         H      SCH.sub.2                                4-Br        5-Cl     H         H      SCH.sub.2                                4-CF.sub.3  5-Cl     H         H      SCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     H         H      SCH.sub.2                                4-OCF.sub.3 5-Cl     H         H      SCH.sub.2                                4-CF.sub.3  4-Cl     H         4-Cl   SCH.sub.2                                4-Cl        4-Cl     H         4-Cl   SCH.sub.2                                4-Br        4-Cl     H         4-Cl   SCH.sub.2                                4-CF.sub.3  4-Cl     H         4-F    SCH.sub.2                                4-Cl        4-Cl     H         4-F    SCH.sub.2                                4-Br        4-Cl     H         4-F    SCH.sub.2                                4-CF.sub.3  5-Cl     H         4-CF.sub.3                                                                            SCH.sub.2                                4-Cl        5-Cl     H         4-CF.sub.3                                                                            SCH.sub.2                                4-Br        5-Cl     H         4-CF.sub.3                                                                            SCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     H         4-CF.sub.3                                                                            SCH.sub.2                                4-CF.sub.3  4-F      Me        4-Cl   SCH.sub.2                                4-Cl        4-F      Me        4-Cl   SCH.sub.2                                4-Br        4-F      Me        4-Cl   SCH.sub.2                                4-OCF.sub.2 H                                                                              4-F      Me        4-Cl   SCH.sub.2                                4-CF.sub.3  4-Cl     Me        4-Cl   SCH.sub.2                                4-Cl        4-Cl     Me        4-Cl   SCH.sub.2                                4-Br        4-Cl     Me        4-Cl   SCH.sub.2                                4-OCF.sub.2 H                                                                              4-Cl     Me        4-Cl   SCH.sub.2                                4-CF.sub.3  5-F      Me        4-F    SCH.sub.2                                4-Cl        5-F      Me        4-F    SCH.sub.2                                4-Br        5-F      Me        4-F    SCH.sub.2                                4-OCF.sub.2 H                                                                              5-F      Me        4-F    SCH.sub.2                                4-CF.sub.3  5-Cl     Me        4-Cl   SCH.sub.2                                4-Cl        5-Cl     Me        4-Cl   SCH.sub.2                                4-Br        5-Cl     Me        4-Cl   SCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   SCH.sub.2                                4-CF.sub.3  5-Cl     Me        4-Cl   SCH.sub.2                                4-Cl        5-Cl     Me        4-Cl   SCH.sub.2                                4-Br        5-Cl     Me        4-Cl   SCH.sub.2                                4-OCF.sub.2 H                                                                              5-Cl     Me        4-Cl   SCH.sub.2                                4-F         5-F      H         H      CH.sub.2 S                               4-Cl        5-F      H         H      CH.sub.2 S                               4-Br        5-F      H         H      CH.sub.2 S                               4-CF.sub.3  5-F      H         H      CH.sub.2 S                               4-OCF.sub.2 H                                                                              5-F      H         H      CH.sub.2 S                               4-OCF.sub.3 5-F      H         H      CH.sub.2 S                               4-CF.sub.3  4-F      H         4-Cl   CH.sub.2 S                               4-Cl        4-F      H         4-Cl   CH.sub.2 S                               4-Br        4-F      H         4-Cl   CH.sub.2 S                               4-CF.sub.3  5-F      H         4-F    CH.sub.2 S                               4-Cl        5-F      H         4-F    CH.sub.2 S                               4-Br        5-F      H         4-F    CH.sub.2 S                               ______________________________________                                    

                  TABLE 12                                                         ______________________________________                                          ##STR20##                                                                     R.sub.1    R.sub.2   R.sub.3    R.sub.4                                                                              A                                        ______________________________________                                         4-CF.sub.3 H         H          H     CH.sub.2                                 4-Cl       H         H          H     CH.sub.2                                 4-Br       H         H          H     CH.sub.2                                 4-OCF.sub.2 H                                                                             H         H          H     CH.sub.2                                 4-OCF.sub.3                                                                               H         H          H     CH.sub.2                                 4-CF.sub.3 4-F       H          H     CH.sub.2                                 4-Cl       4-F       H          H     CH.sub.2                                 4-Br       4-F       H          H     CH.sub.2                                 4-OCF.sub.2 H                                                                             4-F       H          H     CH.sub.2                                 4-OCF.sub.3                                                                               4-F       H          H     CH.sub.2                                 4-CF.sub.3 4-Cl      H          H     CH.sub.2                                 4-Cl       4-Cl      H          H     CH.sub.2                                 4-Br       4-Cl      H          H     CH.sub.2                                 4-OCF.sub.2 H                                                                             4-Cl      H          H     CH.sub.2                                 4-OCF.sub.3                                                                               4-Cl      H          H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-F       H          H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       H          H     CH.sub.2                                 4-CF.sub.3 4-F       Me         H     CH.sub.2                                 4-Cl       4-F       Me         H     CH.sub.2                                 4-Br       4-F       Me         H     CH.sub.2                                 4-OCF.sub.3                                                                               4-F       Me         H     CH.sub.2                                 4-OCF.sub.2 H                                                                             4-F       Me         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      Me         H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Cl      Me         H     CH.sub.2                                 4-CF.sub.3 5-CF.sub.3                                                                               Me         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-CF.sub.3                                                                               Me         H     CH.sub.2                                 4-Cl       5-CF.sub.3                                                                               Me         H     CH.sub.2                                 4-Br       5-CF.sub.3                                                                               Me         H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               Me         H     CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         H     CH.sub.2                                 4-Cl       5-OCF.sub.2 H                                                                            Me         H     CH.sub.2                                 4-Br       5-OCF.sub.2 H                                                                            Me         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            Me         H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            Me         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       Me         H     CH.sub.2                                 4-CF.sub.3 5-Cl      Et         H     CH.sub.2                                 4-Cl       5-Cl      Et         H     CH.sub.2                                 4-Br       5-Cl      Et         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      Et         H     CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            Et         H     CH.sub.2                                 4-Cl       5-OCF.sub.2 H                                                                            Et         H     CH.sub.2                                 4-Br       5-OCF.sub.2 H                                                                            Et         H     CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            Et         H     CH.sub.2                                 4-CF.sub.3 5-F       n-Bu       H     CH.sub.2                                 4-Cl       5-F       n-Bu       H     CH.sub.2                                 4-Br       5-F       n-Bu       H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       n-Bu       H     CH.sub.2                                 4-CF.sub.3 4-F       n-Bu       H     CH.sub.2                                 4-Cl       4-F       n-Bu       H     CH.sub.2                                 4-Br       4-F       n-Bu       H     CH.sub.2                                 4-OCF.sub.3                                                                               4-F       n-Bu       H     CH.sub.2                                 4-CF.sub.3 5-Cl      allyl      H     CH.sub.2                                 4-Cl       5-Cl      allyl      H     CH.sub.2                                 4-Br       5-Cl      allyl      H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       i-Pr       H     CH.sub.2                                 4-CF.sub.3 4-F       i-Pr       H     CH.sub.2                                 4-OCF.sub.3                                                                               4-F       i-Pr       H     CH.sub.2                                 4-CF.sub.3 4-CF.sub.3                                                                               i-Pr       H     CH.sub.2                                 4-OCF.sub.3                                                                               4-CF.sub.3                                                                               i-Pr       H     CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            i-Pr       H     CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            i-Pr       H     CH.sub.2                                 4-CF.sub.3 5-CF.sub.3                                                                               i-Pr       H     CH.sub.2                                 4-OCF.sub.3                                                                               5-CF.sub.3                                                                               i-Pr       H     CH.sub.2                                 4-CF.sub.3 5-Cl      Me         Me    CH.sub.2                                 4-Cl       5-Cl      Me         Me    CH.sub.2                                 4-Br       5-Cl      Me         Me    CH.sub.2                                 4-CF.sub.3 5-F       Me         Me    CH.sub.2                                 4-Cl       5-F       Me         Me    CH.sub.2                                 4-Br       5-F       Me         Me    CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2                                 4-Cl       5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2                                 4-Br       5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2                                 4-CF.sub.3 5-OCF.sub.3                                                                              Me         Me    CH.sub.2                                 4-Cl       5-OCF.sub.3                                                                              Me         Me    CH.sub.2                                 4-Br       5-OCF.sub.3                                                                              Me         Me    CH.sub.2                                 4-CF.sub.3 4-F       Me         Me    CH.sub.2                                 4-Cl       4-F       Me         Me    CH.sub.2                                 4-Br       4-F       Me         Me    CH.sub.2                                 4-CF.sub.3 5-Br      Me         Me    CH.sub.2                                 4-Cl       5-Br      Me         Me    CH.sub.2                                 4-Br       5-Br      Me         Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2                                 4-Cl       5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2                                 4-Br       5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2                                 4-CF.sub.3 5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-Cl       5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-Br       5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2                                 4-CF.sub.3 5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2                                 4-Cl       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2                                 4-Br       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Cl       5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Br       5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Cl       5-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Br       5-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Cl       4-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Br       4-F       CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Cl       4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-Br       4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               H     CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                H         CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 C(Me).sub.2 O                                                                5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                5-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                4-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                5-Me      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-Br      CO.sub.2 Me                                                                               Me    CH.sub. 2                                4-OCF.sub.3                                                                               5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                5-Br      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CF.sub.2 CF.sub.2 O                                                                   5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub.2                                 3,4-CH.sub.2 C(Me).sub.2 O                                                                5-OCF.sub.3                                                                              CO.sub.2 Me                                                                               Me    CH.sub. 2                                4-CF.sub.3 5-CN      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       5-CN      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       5-CN      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             5-CN      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-CN      CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 6-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Cl       6-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-Br       6-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.2 H                                                                             6-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-OCF.sub.3                                                                               6-F       CO.sub.2 Me                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Et    CH.sub.2                                 4-Cl       5-Cl      CO.sub.2 Me                                                                               Et    CH.sub.2                                 4-Br       5-Cl      CO.sub.2 Me                                                                               Et    CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          CH.sub.2                                 4-Cl       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          CH.sub.2                                 4-Br       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               allyl CH.sub.2                                 4-Cl       5-Cl      CO.sub.2 Me                                                                               allyl CH.sub.2                                 4-Br       5-Cl      CO.sub.2 Me                                                                               allyl CH.sub.2                                 4-CF.sub.3 5-F       CO.sub.2 Et                                                                               Me    CH.sub.2                                 4-Cl       5-F       CO.sub.2 Et                                                                               Me    CH.sub.2                                 4-Br       5-F       CO.sub.2 Et                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    CH.sub.2                                 4-Cl       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    CH.sub.2                                 4-Br       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    CH.sub.2                                 4-CF.sub.3 5-F       CO.sub.2 Ph                                                                               Me    CH.sub.2                                 4-Cl       5-F       CO.sub.2 Ph                                                                               Me    CH.sub.2                                 4-Br       5-F       CO.sub.2 Ph                                                                               Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CO.sub.2 H H     CH.sub.2                                 4-CF.sub.3 5-Cl      CONHMe     H     CH.sub.2                                 4-CF.sub.3 5-Cl      CONMe      H     CH.sub.2                                 4-CF.sub.3 5-Cl      CONHPh     H     CH.sub.2                                 4-CF.sub.3 5-Cl      CSNMe.sub.2                                                                               H     CH.sub.2                                 4-CF.sub.3 5-Cl      propargyl  Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CH.sub.2 CH.sub.2 CN                                                                      Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CH.sub.2 CO.sub.2 Me                                                                      Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CH.sub.2 OMe                                                                              Me    CH.sub.2                                 4-CF.sub.3 5-Cl      OMe        H     CH.sub.2                                 4-CF.sub.3 5-Cl      SMe        H     CH.sub.2                                 4-CF.sub.3 5-Cl      SO.sub.2 Me                                                                               H     CH.sub.2                                 4-CF.sub.3 5-Cl      C(O)Me     Me    CH.sub.2                                 4-CF.sub.3 5-Cl      C(O)Et     Me    CH.sub.2                                 4-CF.sub.3 5-Cl      C(O)Me     H     CH.sub.2                                 4-CF.sub.3 5-Cl      C(O)Et     H     CH.sub. 2                                4-CF.sub.3 5-Cl      CN         Me    CH.sub.2                                 4-CF.sub.3 5-Cl      CN         Et    CH.sub.2                                 4-CF.sub.3 5-Cl      CN         CH.sub.2 Ph                                                                          CH.sub.2                                 4-CF.sub.3 5-Cl      CN         H     CH.sub.2                                 4-CF.sub.3 H         H          H     CH.sub.2 CH.sub.2                        4-Cl       H         H          H     CH.sub.2 CH.sub.2                        4-Br       H         H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             H         H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-F       H          H     CH.sub.2 CH.sub.2                        4-Cl       4-F       H          H     CH.sub.2 CH.sub.2                        4-Br       4-F       H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             4-F       H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-Cl      H          H     CH.sub.2 CH.sub.2                        4-Cl       4-Cl      H          H     CH.sub.2 CH.sub.2                        4-Br       4-Cl      H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             4-Cl      H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       H          H     CH.sub.2 CH.sub.2                        4-Cl       5-F       H          H     CH.sub.2 CH.sub.2                        4-Br       5-F       H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-F       H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 6-F       H          H     CH.sub.2 CH.sub.2                        4-Cl       6-F       H          H     CH.sub.2 CH.sub.2                        4-Br       6-F       H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             6-F       H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 6-Cl      H          H     CH.sub.2 CH.sub.2                        4-Cl       6-Cl      H          H     CH.sub.2 CH.sub.2                        4-Br       6-Cl      H          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             6-Cl      H          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-F       Me         H     CH.sub.2 CH.sub.2                        4-Cl       4-F       Me         H     CH.sub.2 CH.sub.2                        4-Br       4-F       Me         H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             4-F       Me         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      Me         H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      Me         H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      Me         H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-Cl      Me         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         H     CH.sub.2 CH.sub.2                        4-Cl       5-OCF.sub.2 H                                                                            Me         H     CH.sub.2 CH.sub.2                        4-Br       5-OCF.sub.2 H                                                                            Me         H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            Me         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       Me         H     CH.sub.2 CH.sub.2                        4-Cl       5-F       Me         H     CH.sub.2 CH.sub.2                        4-Br       5-F       Me         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      Et         H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      Et         H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      Et         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Et         H     CH.sub.2 CH.sub.2                        4-Cl       5-OCF.sub.2 H                                                                            Et         H     CH.sub.2 CH.sub.2                        4-Br       5-OCF.sub.2 H                                                                            Et         H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-Cl       5-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-Br       5-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-Cl       4-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-Br       4-F       n-Bu       H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      allyl      H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      allyl      H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      allyl      H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      Me         Me    CH.sub.2 CH.sub.2                        4-Cl       5-Cl      Me         Me    CH.sub.2 CH.sub.2                        4-Br       5-Cl      Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       Me         Me    CH.sub.2 CH.sub.2                        4-Cl       5-F       Me         Me    CH.sub.2 CH.sub.2                        4-Br       5-F       Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2 CH.sub.2                        4-Cl       5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2 CH.sub.2                        4-Br       5-OCF.sub.2 H                                                                            Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-OCF.sub.3                                                                              Me         Me    CH.sub.2 CH.sub. 2                       4-Cl       5-OCF.sub.3                                                                              Me         Me    CH.sub.2 CH.sub.2                        4-Br       5-OCF.sub.3                                                                              Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 4-F       Me         Me    CH.sub.2 CH.sub.2                        4-Cl       4-F       Me         Me    CH.sub.2 CH.sub.2                        4-Br       4-F       Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Br      Me         Me    CH.sub.2 CH.sub.2                        4-Cl       5-Br      Me         Me    CH.sub.2 CH.sub.2                        4-Br       5-Br      Me         Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-Cl       5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-Br       5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     CH.sub.2 CH.sub.2                        4-CF.sub.3 H         CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       H         CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Br       H         CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-F        H         CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Br       5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-NO.sub.2 5-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Br       5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CN       5-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       4-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Br       4-F       CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Cl       4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-Br       4-Cl      CO.sub.2 Me                                                                               H     CH.sub.2 CH.sub.2                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-Br       5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-Cl      CO.sub. 2 Me                                                                              Me    CH.sub.2 CH.sub.2                        3,4-CF.sub.2 C(Me).sub.2 O                                                                5-Cl      CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-Cl       5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-Br       5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        3,4-CH.sub.2 C(Me).sub.2 O                                                                5-F       CO.sub.2 Me                                                                               Me    CH.sub.2 CH.sub.2                        4-CF.sub.3 H         H          H     O                                        4-Cl       H         H          H     O                                        4-Br       H         H          H     O                                        4-OCF.sub.3                                                                               H         H          H     O                                        4-OCF.sub.2 H                                                                             H         H          H     O                                        4-CF.sub.3 4-F       H          H     O                                        4-Cl       4-F       H          H     O                                        4-Br       4-F       H          H     O                                        4-OCF.sub.3                                                                               4-F       H          H     O                                        4-OCF.sub.2 H                                                                             4-F       H          H     O                                        4-CF.sub.3 4-Cl      H          H     O                                        4-Cl       4-Cl      H          H     O                                        4-Br       4-Cl      H          H     O                                        4-OCF.sub.3                                                                               4-Cl      H          H     O                                        4-OCF.sub.2 H                                                                             4-Cl      H          H     O                                        4-CF.sub.3 5-F       H          H     O                                        4-Cl       5-F       H          H     O                                        4-Br       5-F       H          H     O                                        4-OCF.sub.3                                                                               5-F       H          H     O                                        4-OCF.sub.2 H                                                                             5-F       H          H     O                                        4-CF.sub.3 6-F       H          H     O                                        4-CF.sub.3 4-F       Me         H     O                                        4-Cl       4-F       Me         H     O                                        4-Br       4-F       Me         H     O                                        4-OCF.sub.3                                                                               4-F       Me         H     O                                        4-OCF.sub.2 H                                                                             4-F       Me         H     O                                        4-CF.sub.3 5-Cl      Me         H     O                                        4-Cl       5-Cl      Me         H     O                                        4-Br       5-Cl      Me         H     O                                        4-OCF.sub.3                                                                               5-Cl      Me         H     O                                        4-OCF.sub.2 H                                                                             5-Cl      Me         H     O                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         H     O                                        4-Cl       5-OCF.sub.2 H                                                                            Me         H     O                                        4-Br       5-OCF.sub.2 H                                                                            Me         H     O                                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            Me         H     O                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            Me         H     O                                        4-CF.sub.3 5-CF.sub.3                                                                               Me         H     O                                        4-Cl       5-CF.sub.3                                                                               Me         H     O                                        4-Br       5-CF.sub.3                                                                               Me         H     O                                        4-OCF.sub.3                                                                               5-CF.sub.3                                                                               Me         H     O                                        4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               Me         H     O                                        4-CF.sub.3 5-F       Me         H     O                                        4-Cl       5-F       Me         H     O                                        4-Br       5-F       Me         H     O                                        4-OCF.sub.3                                                                               5-F       Me         H     O                                        4-CF.sub.3 5-Cl      Et         H     O                                        4-Cl       5-Cl      Et         H     O                                        4-Br       5-Cl      Et         H     O                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Et         H     O                                        4-Cl       5-OCF.sub.2 H                                                                            Et         H     O                                        4-Br       5-OCF.sub.2 H                                                                            Et         H     O                                        4-CF.sub.3 5-F       n-Bu       H     O                                        4-Cl       5-F       n-Bu       H     O                                        4-Br       5-F       n-Bu       H     O                                        4-CF.sub.3 4-F       n-Bu       H     O                                        4-Cl       4-F       n-Bu       H     O                                        4-Br       4-F       n-Bu       H     O                                        4-CF.sub.3 5-Cl      allyl      H     O                                        4-Cl       5-Cl      allyl      H     O                                        4-Br       5-Cl      allyl      H     O                                        4-CF.sub.3 5-Cl      Me         Me    O                                        4-Cl       5-Cl      Me         Me    O                                        4-Br       5-Cl      Me         Me    O                                        4-CF.sub.3 5-F       Me         Me    O                                        4-Cl       5-F       Me         Me    O                                        4-Br       5-F       Me         Me    O                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         Me    O                                        4-Cl       5-OCF.sub.2 H                                                                            Me         Me    O                                        4-Br       5-OCF.sub.2 H                                                                            Me         Me    O                                        4-CF.sub.3 5-OCF.sub.3                                                                              Me         Me    O                                        4-Cl       5-OCF.sub.3                                                                              Me         Me    O                                        4-Br       5-OCF.sub.3                                                                              Me         Me    O                                        4-CF.sub.3 4-F       Me         Me    O                                        4-Cl       4-F       Me         Me    O                                        4-Br       4-F       Me         Me    O                                        4-CF.sub.3 5-Br      Me         Me    O                                        4-Cl       5-Br      Me         Me    O                                        4-Br       5-Br      Me         Me    O                                        4-OCF.sub.3                                                                               5-Cl      allyl      Me    O                                        4-CF.sub.3 5-F       allyl      Me    O                                        4-OCF.sub.3                                                                               5-F       allyl      Me    O                                        4-CF.sub.3 5-F       Et         Me    O                                        4-OCF.sub.3                                                                               5-F       Et         Me    O                                        4-CF.sub.3 5-Cl      Et         Me    O                                        4-OCF.sub.3                                                                               5-Cl      Et         Me    O                                        4-CF.sub.3 5-CF.sub.3                                                                               Et         Me    O                                        4-CF.sub.3 5-CF.sub.3                                                                               allyl      Me    O                                        4-OCF.sub.3                                                                               5-CF.sub.3                                                                               allyl      Me    O                                        4-CF.sub.3 5-F       CH.sub.2 Ph                                                                               Me    O                                        4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph                                                                               Me    O                                        4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               Me    O                                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               Me    O                                        4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               H     O                                        4-Cl       5-Cl      CH.sub.2 Ph                                                                               H     O                                        4-Br       5-Cl      CH.sub.2 Ph                                                                               H     O                                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               H     O                                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph                                                                               H     O                                        4-CF.sub.3 5-F       CH.sub.2 Ph-4-F                                                                           H     O                                        4-Cl       5-F       CH.sub.2 Ph-4-F                                                                           H     O                                        4-Br       5-F       CH.sub.2 Ph-4-F                                                                           H     O                                        4-OCF.sub.2 H                                                                             5-F       CH.sub.2 Ph-4-F                                                                           H     O                                        4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph-4-F                                                                           H     O                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     O                                        4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     O                                        4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     O                                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     O                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     O                                        4-CF.sub.3 5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     O                                        4-Cl       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     O                                        4-Br       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     O                                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     O                                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     O                                        4-CF.sub.3 H         CO.sub.2 Me                                                                               H     O                                        4-Cl       H         CO.sub.2 Me                                                                               H     O                                        4-Br       H         CO.sub.2 Me                                                                               H     O                                        4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               H     O                                        4-F        H         CO.sub.2 Me                                                                               H     O                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     O                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               H     O                                        4-Br       5-Cl      CO.sub.2 Me                                                                               H     O                                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               H     O                                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     O                                        4-NO.sub.2 5-Cl      CO.sub.2 Me                                                                               H     O                                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     O                                        4-Cl       5-F       CO.sub.2 Me                                                                               H     O                                        4-Br       5-F       CO.sub.2 Me                                                                               H     O                                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     O                                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     O                                        4-CN       5-F       CO.sub.2 Me                                                                               H     O                                        4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     O                                        4-Cl       4-F       CO.sub.2 Me                                                                               H     O                                        4-Br       4-F       CO.sub.2 Me                                                                               H     O                                        4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     O                                        4-Cl       4-Cl      CO.sub.2 Me                                                                               H     O                                        4-Br       4-Cl      CO.sub. 2 Me                                                                              H     O                                        4-CF.sub.3 H         CO.sub.2 Me                                                                               Me    O                                        4-Cl       H         CO.sub.2 Me                                                                               Me    O                                        4-Br       H         CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               H         CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    O                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    O                                        4-Br       5-Cl      CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    O                                        4-Cl       5-F       CO.sub.2 Me                                                                               Me    O                                        4-Br       5-F       CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 4-F       CO.sub.2 Me                                                                               Me    O                                        4-Cl       4-F       CO.sub.2 Me                                                                               Me    O                                        4-Br       4-F       CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               Me    O                                        3,4-CF.sub.2 CF.sub.2 O                                                                   4-F       CO.sub.2 Me                                                                               Me    O                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                4-F       CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    O                                        4-Cl       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    O                                        4-Br       5-CF.sub. 3                                                                              CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-Br      CO.sub.2 Me                                                                               Me    O                                        4-Cl       5-Br      CO.sub.2 Me                                                                               Me    O                                        4-Br       5-Br      CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               5-Br      CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             5-Br      CO.sub.2 Me                                                                               Me    O                                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-Br      CO.sub.2 Me                                                                               Me    O                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                5-Br      CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    O                                        4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    O                                        4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    O                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    O                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Et    O                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               Et    O                                        4-Br       5-Cl      CO.sub.2 Me                                                                               Et    O                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          O                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          O                                        4-Br       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          O                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               allyl O                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               allyl O                                        4-Br       5-Cl      CO.sub.2 Me                                                                               allyl O                                        4-CF.sub.3 5-F       CO.sub.2 Et                                                                               Me    O                                        4-Cl       5-F       CO.sub.2 Et                                                                               Me    O                                        4-Br       5-F       CO.sub.2 Et                                                                               Me    O                                        4-CF.sub.3 5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    O                                        4-Cl       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    O                                        4-Br       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    O                                        4-CF.sub.3 5-F       CO.sub.2 Ph                                                                               Me    O                                        4-Cl       5-F       CO.sub.2 Ph                                                                               Me    O                                        4-Br       5-F       CO.sub.2 Ph                                                                               Me    O                                        4-CF.sub.3 5-Cl      CO.sub.2 H H     O                                        4-CF.sub.3 5-Cl      CONHMe     H     O                                        4-CF.sub.3 5-Cl      CONMe      H     O                                        4-CF.sub.3 5-Cl      CONHPh     H     O                                        4-CF.sub.3 5-Cl      CSNMe.sub.2                                                                               H     O                                        4-CF.sub.3 5-Cl      propargyl  Me    O                                        4-CF.sub.3 5-Cl      CH.sub.2 CH.sub.2 CN                                                                      Me    O                                        4-CF.sub.3 5-Cl      CH.sub.2 CO.sub.2 Me                                                                      Me    O                                        4-CF.sub.3 5-Cl      CH.sub.2 OMe                                                                              Me    O                                        4-CF.sub.3 5-Cl      OMe        H     O                                        4-CF.sub.3 5-Cl      SMe        H     O                                        4-CF.sub.3 5-Cl      SO.sub.2 Me                                                                               H     O                                        4-CF.sub.3 5-Cl      C(O)Me     Me    O                                        4-CF.sub.3 5-Cl      C(O)Et     Me    O                                        4-CF.sub.3 5-Cl      C(O)Me     H     O                                        4-CF.sub.3 5-Cl      C(O)Et     H     O                                        4-CF.sub.3 5-Cl      CN         Me    O                                        4-CF.sub.3 5-Cl      CN         Et    O                                        4-CF.sub.3 5-Cl      CN         CH.sub.2 Ph                                                                          O                                        4-CF.sub.3 5-Cl      CN         H     O                                        4-CF.sub.3 H         H          H     S                                        4-Cl       H         H          H     S                                        4-Br       H         H          H     S                                        4-OCF.sub.2 H                                                                             H         H          H     S                                        4-CF.sub.3 4-F       H          H     S                                        4-Cl       4-F       H          H     S                                        4-Br       4-F       H          H     S                                        4-OCF.sub.2 H                                                                             4-F       H          H     S                                        4-CF.sub.3 4-Cl      H          H     S                                        4-Cl       4-Cl      H          H     S                                        4-Br       4-Cl      H          H     S                                        4-OCF.sub.2 H                                                                             4-Cl      H          H     S                                        4-CF.sub.3 5-F       H          H     S                                        4-Cl       5-F       H          H     S                                        4-Br       5-F       H          H     S                                        4-OCF.sub.2 H                                                                             5-F       H          H     S                                        4-CF.sub.3 4-F       Me         H     S                                        4-Cl       4-F       Me         H     S                                        4-Br       4-F       Me         H     S                                        4-OCF.sub.2 H                                                                             4-F       Me         H     S                                        4-CF.sub.3 5-Cl      Me         H     S                                        4-Cl       5-Cl      Me         H     S                                        4-Br       5-Cl      Me         H     S                                        4-OCF.sub.2 H                                                                             5-Cl      Me         H     S                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         H     S                                        4-Cl       5-OCF.sub.2 H                                                                            Me         H     S                                        4-Br       5-OCF.sub.2 H                                                                            Me         H     S                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            Me         H     S                                        4-CF.sub.3 5-F       Me         H     S                                        4-Cl       5-F       Me         H     S                                        4-Br       5-F       Me         H     S                                        4-CF.sub.3 5-Cl      Et         H     S                                        4-Cl       5-Cl      Et         H     S                                        4-Br       5-Cl      Et         H     S                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Et         H     S                                        4-Cl       5-OCF.sub.2 H                                                                            Et         H     S                                        4-Br       5-OCF.sub.2 H                                                                            Et         H     S                                        4-CF.sub.3 5-F       n-Bu       H     S                                        4-Cl       5-F       n-Bu       H     S                                        4-Br       5-F       n-Bu       H     S                                        4-CF.sub.3 4-F       n-Bu       H     S                                        4-Cl       4-F       n-Bu       H     S                                        4-Br       4-F       n-Bu       H     S                                        4-CF.sub.3 5-Cl      allyl      H     S                                        4-Cl       5-Cl      allyl      H     S                                        4-Br       5-Cl      allyl      H     S                                        4-CF.sub.3 5-Cl      Me         Me    S                                        4-Cl       5-Cl      Me         Me    S                                        4-Br       5-Cl      Me         Me    S                                        4-CF.sub.3 5-F       Me         Me    S                                        4-Cl       5-F       Me         Me    S                                        4-Br       5-F       Me         Me    S                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         Me    S                                        4-Cl       5-OCF.sub.2 H                                                                            Me         Me    S                                        4-Br       5-OCF.sub.2 H                                                                            Me         Me    S                                        4-CF.sub.3 5-OCF.sub.3                                                                              Me         Me    S                                        4-Cl       5-OCF.sub.3                                                                              Me         Me    S                                        4-Br       5-OCF.sub.3                                                                              Me         Me    S                                        4-CF.sub.3 4-F       Me         Me    S                                        4-Cl       4-F       Me         Me    S                                        4-Br       4-F       Me         Me    S                                        4-CF.sub.3 5-Br      Me         Me    S                                        4-Cl       5-Br      Me         Me    S                                        4-Br       5-Br      Me         Me    S                                        4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               H     S                                        4-Cl       5-Cl      CH.sub. 2 Ph                                                                              H     S                                        4-Br       5-Cl      CH.sub.2 Ph                                                                               H     S                                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               H     S                                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph                                                                               H     S                                        4-CF.sub.3 5-F       CH.sub.2 Ph-4-F                                                                           H     S                                        4-Cl       5-F       CH.sub.2 Ph-4-F                                                                           H     S                                        4-Br       5-F       CH.sub.2 Ph-4-F                                                                           H     S                                        4-OCF.sub.2 H                                                                             5-F       CH.sub.2 Ph-4-F                                                                           H     S                                        4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph-4-F                                                                           H     S                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     S                                        4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     S                                        4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     S                                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     S                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-F                                                                           H     S                                        4-CF.sub.3 5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     S                                        4-Cl       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     S                                        4-Br       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     S                                        4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     S                                        4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     S                                        4-CF.sub.3 H         CO.sub.2 Me                                                                               H     S                                        4-Cl       H         CO.sub.2 Me                                                                               H     S                                        4-Br       H         CO.sub.2 Me                                                                               H     S                                        4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               H     S                                        4-F        H         CO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     S                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               H     S                                        4-Br       5-Cl      CO.sub.2 Me                                                                               H     S                                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               H     S                                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     S                                        4-NO.sub.2 5-Cl      CO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     S                                        4-Cl       5-F       CO.sub.2 Me                                                                               H     S                                        4-Br       5-F       CO.sub.2 Me                                                                               H     S                                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     S                                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     S                                        4-CN       5-F       CO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     S                                        4-Cl       4-F       CO.sub.2 Me                                                                               H     S                                        4-Br       4-F       CO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     S                                        4-Cl       4-Cl      CO.sub.2 Me                                                                               H     S                                        4-Br       4-Cl      CO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 H         CO.sub.2 Me                                                                               Me    S                                        4-Cl       H         CO.sub.2 Me                                                                               Me    S                                        4-Br       H         CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             H         CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               H         CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 CF.sub.2 O                                                                   H         CO.sub.2 Me                                                                               Me    S                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                H         CO.sub.2 Me                                                                               Me    S                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    S                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    S                                        4-Br       5-Cl      CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-Cl      CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 C(Me).sub.2 O                                                                5-Cl      CO.sub.2 Me                                                                               Me    S                                        4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    S                                        4-Cl       5-F       CO.sub.2 Me                                                                               Me    S                                        4-Br       5-F       CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-F       CO.sub.2 Me                                                                               Me    S                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                5-F       CO.sub.2 Me                                                                               Me    S                                        4-CF.sub.3 4-F       CO.sub.2 Me                                                                               Me    S                                        4-Cl       4-F       CO.sub.2 Me                                                                               Me    S                                        4-Br       4-F       CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 CF.sub.2 O                                                                   4-F       CO.sub.2 Me                                                                               Me    S                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                4-F       CO.sub.2 Me                                                                               Me    S                                        4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        3,4-CF.sub.2 CF.sub.2 O                                                                   5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        3,4-CH.sub.2 C(Me).sub.2 O                                                                5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.2 H                                                                             6-F       CO.sub.2 Me                                                                               Me    S                                        4-OCF.sub.3                                                                               6-F       CO.sub.2 Me                                                                               Me    S                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Et    S                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               Et    S                                        4-Br       5-Cl      CO.sub.2 Me                                                                               Et    S                                        4-CF.sub.3 5-Cl      Co.sub.2 Me                                                                               CH.sub.2 Ph                                                                          S                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          S                                        4-Br       5-Cl      CO.sub.2 Me                                                                               CH.sub.2 Ph                                                                          S                                        4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               allyl S                                        4-Cl       5-Cl      CO.sub.2 Me                                                                               allyl S                                        4-Br       5-Cl      CO.sub.2 Me                                                                               allyl S                                        4-CF.sub.3 5-F       CO.sub.2 Et                                                                               Me    S                                        4-Cl       5-F       CO.sub.2 Et                                                                               Me    S                                        4-Br       5-F       CO.sub.2 Et                                                                               Me    S                                        4-CF.sub.3 5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    S                                        4-Cl       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    S                                        4-Br       5-F       CO.sub.2 CH.sub.2 CF.sub.3                                                                Me    S                                        4-CF.sub.3 5-F       CO.sub.2 Ph                                                                               Me    S                                        4-Cl       5-F       CO.sub. 2 Ph                                                                              Me    S                                        4-Br       5-F       CO.sub.2 Ph                                                                               Me    S                                        4-CF.sub.3 5-Cl      CO.sub.2 H H     S                                        4-CF.sub.3 5-Cl      CONHMe     H     S                                        4-CF.sub.3 5-Cl      CONMe      H     S                                        4-CF.sub.3 5-Cl      CONHPh     H     S                                        4-CF.sub.3 5-Cl      CSNMe.sub.2                                                                               H     S                                        4-CF.sub.3 5-Cl      propargyl  Me    S                                        4-CF.sub.3 5-Cl      CH.sub.2 CH.sub.2 CN                                                                      Me    S                                        4-CF.sub.3 5-Cl      CH.sub.2 CO.sub.2 Me                                                                      Me    S                                        4-CF.sub.3 5-Cl      CH.sub.2 OMe                                                                              Me    S                                        4-CF.sub.3 5-Cl      OMe        H     S                                        4-CF.sub.3 5-Cl      SMe        H     S                                        4-CF.sub.3 5-Cl      SO.sub.2 Me                                                                               H     S                                        4-CF.sub.3 5-Cl      C(O)Me     Me    S                                        4-CF.sub.3 5-Cl      C(O)Et     Me    S                                        4-CF.sub.3 5-Cl      C(O)Me     H     S                                        4-CF.sub.3 5-Cl      C(O)Et     H     S                                        4-CF.sub.3 5-Cl      CN         Me    S                                        4-CF.sub.3 5-Cl      CN         Et    S                                        4-CF.sub.3 5-Cl      CN         CH.sub.2 Ph                                                                          S                                        4-CF.sub.3 5-Cl      CN         H     S                                        4-CF.sub.3 4-F       allyl      H     OCH.sub.2                                4-Cl       4-F       allyl      H     OCH.sub.2                                4-Br       4-F       allyl      H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       allyl      H     OCH.sub.2                                4-OCF.sub.3                                                                               4-F       allyl      H     OCH.sub.2                                4-CF.sub.3 4-Cl      allyl      H     OCH.sub.2                                4-Cl       4-Cl      allyl      H     OCH.sub.2                                4-Br       4-Cl      allyl      H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      allyl      H     OCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      allyl      H     OCH.sub.2                                4-CF.sub.3 5-F       propargyl  H     OCH.sub.2                                4-Cl       5-F       propargyl  H     OCH.sub.2                                4-Br       5-F       propargyl  H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       propargyl  H     OCH.sub.2                                4-OCF.sub.3                                                                               5-F       propargyl  H     OCH.sub.2                                4-CF.sub.3 5-Cl      Me         H     OCH.sub.2                                4-Cl       5-Cl      Me         H     OCH.sub.2                                4-Br       5-Cl      Me         H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      Me         H     OCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      Me         H     OCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               Me         H     OCH.sub.2                                4-Cl       5-CF.sub.3                                                                               Me         H     OCH.sub.2                                4-Br       5-CF.sub.3                                                                               Me         H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               Me         H     OCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               Me         H     OCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            Me         H     OCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            Me         H     OCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            Me         H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            Me         H     OCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            Me         H     OCH.sub.2                                4-CF.sub.3 4-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Cl       4-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Br       4-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               4-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-CF.sub.3 4-Cl      CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Cl       4-Cl      CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Br       4-Cl      CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-CF.sub.3 5-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Cl       5-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-Br       5-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               5-F       CH.sub.2 Ph                                                                               H     OCH.sub.2                                4-CF.sub.3 5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Cl       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Br       5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Br       5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     OCH.sub.2                                4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       4-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       4-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       4-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       4-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       5-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       5-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       5-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       5-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub. 2 H                                                                            5-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     OCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     OCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     OCH.sub.2                                4-CF.sub.3 4-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       4-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       4-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       4-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       4-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       5-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       5-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       5-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    OCH.sub.2                                4-CF.sub.3 4-F       Me         H     SCH.sub.2                                4-Cl       4-F       Me         H     SCH.sub.2                                4-Br       4-F       Me         H     SCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       Me         H     SCH.sub.2                                4-OCF.sub.3                                                                               4-F       Me         H     SCH.sub.2                                4-CF.sub.3 4-Cl      Me         H     SCH.sub.2                                4-Cl       4-Cl      Me         H     SCH.sub.2                                4-Br       4-Cl      Me         H     SCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      Me         H     SCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      Me         H     SCH.sub.2                                4-CF.sub.3 5-F       allyl      H     SCH.sub.2                                4-Cl       5-F       allyl      H     SCH.sub.2                                4-Br       5-F       allyl      H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       allyl      H     SCH.sub.2                                4-OCF.sub.3                                                                               5-F       allyl      H     SCH.sub.2                                4-CF.sub.3 5-Cl      CH.sub.2 Ph                                                                               H     SCH.sub.2                                4-Cl       5-Cl      CH.sub.2 Ph                                                                               H     SCH.sub.2                                4-Br       5-Cl      CH.sub.2 Ph                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      CH.sub.2 Ph                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CH.sub.2 Ph                                                                               H     SCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-Br       5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CH.sub.2 Ph-4-Cl                                                                          H     SCH.sub.2                                4-CF.sub.3 4-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       4-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       4-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       4-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       4-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 5-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       5-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       5-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       5-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       5-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     SCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     SCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               H     SCH.sub.2                                4-CF.sub.3 4-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       4-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       4-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             4-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               4-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-CF.sub.3 4-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       4-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       4-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             4-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               4-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-CF.sub.3 5-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       5-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       5-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             5-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               5-F       CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-CF.sub.3 5-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       5-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       5-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             5-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               5-Cl      CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-CF.sub.3 5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               5-CF.sub.3                                                                               CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-CF.sub.3 5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Cl       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-Br       5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.2 H                                                                             5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    SCH.sub.2                                4-OCF.sub.3                                                                               5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               Me    SCH.sub.2                                ______________________________________                                    

                                      TABLE 13                                     __________________________________________________________________________      ##STR21##                                                                     R.sub.1                                                                            R.sub.2                                                                           R.sub.3                                                                             R.sub.4                                                                           R.sub.5     R.sub.6  A                                          __________________________________________________________________________     4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  Me          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  Me          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  Me          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  C(O)Me      H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  C(O)Me      H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  C(O)Me      H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  CO.sub.2 Me H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  CO.sub.2 Me H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  CO.sub.2 Me H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  Ph          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  Ph          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  Ph          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  4-ClPh      H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  4-ClPh      H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  4-ClPh      H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  4-FPh       H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  4-FPh       H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  5-FPh       H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  Me          H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  Me          H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  Me          H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  Ph          H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  Ph          H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  Ph          H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  SN(Me)CO.sub.2 n-Bu                                                                        H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  SN(Me)CO.sub.2 n-Bu                                                                        H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  SN(Me)CO.sub.2 n-Bu                                                                        H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  SN(i-Pr)CO.sub.2 Et                                                                        H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  SN(i-Pr)CO.sub.2 Et                                                                        H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  SN(i-Pr)CO.sub.2 Et                                                                        H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  SCO.sub.2 n-Hex                                                                            H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  SCO.sub.2 n-Hex                                                                            H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  SCO.sub.2 n-Hex                                                                            H        CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  SN(Me)SO.sub.2 Me                                                                          H        CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  SN(Me)SO.sub.2 Me                                                                          H        CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  SN(Me)SO.sub.2 Me                                                                          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  Me          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  4-FPh       H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  4-FPh       H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  4-FPh       H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  SPh         H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  SPh         H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  SPh         H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  CO.sub.2 Et H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  CO.sub.2 Et H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  CO.sub.2 Et H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  SCO.sub.2 n-Bu                                                                             H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  SCO.sub.2 n-Bu                                                                             H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  SCO.sub.2 n-Bu                                                                             H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  SMe         H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  SMe         H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  SMe         H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  CO.sub.2 Me H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  CO.sub.2 Me H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  CO.sub.2 Me H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  SN(Me)SO.sub.2 -4-MePh                                                                     H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  SN(Me)SO.sub.2 -4-MePh                                                                     H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  SN(Me)SO.sub.2 -4-MePh                                                                     H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  SN(Me)P(O)(OEt).sub.2                                                                      H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  SN(Me)P(O)(OEt).sub.2                                                                      H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  SN(Me)P(O)(OEt).sub.2                                                                      H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H                                                                                  ##STR22##  H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H                                                                                  ##STR23##  H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H                                                                                  ##STR24##  H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-F Ph                                                                              H  CO.sub.2 Et H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  CO.sub.2 Et H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  CO.sub.2 Et H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  Ph          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  Ph          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  Ph          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           C(O)Me   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           C(O)Me   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           C(O)Me   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           C(O)Ph   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           C(O)Ph   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           C(O)Ph   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  H           C(O)nPr  CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  H           C(O)nPr  CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  H           C(O)nPr  CH.sub.2                                   4-CF3                                                                              5-F                                                                               Ph   H  H           CH.sub.2 Ph                                                                             CH2                                        4-Cl                                                                               5-F                                                                               Ph   H  H           CH.sub.2 Ph                                                                             CH2                                        4-Br                                                                               5-F                                                                               Ph   H  H           CH.sub.2 Ph                                                                             CH2                                        4-CF.sub.3                                                                         5-F                                                                               Ph   H  H           SN(Me)CO.sub.2 n-dec                                                                    CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  H           SN(Me)CO.sub.2 n-dec                                                                    CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  H           SN(Me)CO.sub.2 n-dec                                                                    CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  H           SN(i-Pr)CO.sub.2 Et                                                                     CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  H           SN(i-Pr)CO.sub.2 Et                                                                     CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  H           SN(i-Pr)CO.sub.2 Et                                                                     CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  H           SCO.sub.2 Et                                                                            CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  H           SCO.sub.2 Et                                                                            CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  H           SCO.sub.2 Et                                                                            CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  H           C(O)Me   CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  H           C(O)Me   CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  H           C(O)Me   CH.sub.2                                   4-CF.sub.3                                                                         5-F                                                                               Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-F                                                                               Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-F                                                                               Ph   H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-Cl Ph                                                                             H  H           Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           CO.sub.2 Et                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  H           C(O)Me   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           C(O)Me   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           C(O)Me   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  H           SN(Et).sub.2                                                                            CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           SN(Et).sub.2                                                                            CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           SN(Et).sub.2                                                                            CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  H           SO.sub.2 Ph                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           SO.sub.2 Ph                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  H           SO.sub.2 Ph                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           C(O)Me   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           C(O)Me   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           C(O)Me   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           n-Bu     CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           n-Bu     CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           n-Bu     CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           SN(Me)CO.sub.2 Et                                                                       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           SN(Me)CO.sub.2 Et                                                                       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           SN(Me)CO.sub.2 Et                                                                       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-FPh                                                                               H  H           C(O)Ph   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-FPh                                                                               H  H           C(O)Ph   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-FPh                                                                               H  H           C(O)Ph   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me H           Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me Me          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me Me          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me Me          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me Ph          H        CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me Ph          H        CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me Ph          H        CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me H           C(O)Me   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           C(O)Me   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           C(O)Me   CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              Me H           SCO.sub.2 Me                                                                            CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           SCO.sub.2 Me                                                                            CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              Me H           SCO.sub.2 Me                                                                            CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  Me          Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  Me          C(O)Me   CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          C(O)Me   CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  Me          C(O)Me   CH.sub. 2                                  4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  Ph          Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  Ph          Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  Ph          Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              4-ClPh                                                                              H  Ph          CO.sub.2 Me                                                                             CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              4-ClPh                                                                              H  Ph          CO.sub.2 Me                                                                             CH.sub.2                                   4-Br                                                                               5-Cl                                                                              4-ClPh                                                                              H  Ph          CO.sub.2 Me                                                                             CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  Me          Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  Me          Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  Me          Me       CH.sub.2                                   4-CF.sub.3                                                                         5-Cl                                                                              Ph   H  CO.sub.2 Me Me       CH.sub.2                                   4-Cl                                                                               5-Cl                                                                              Ph   H  CO.sub.2 Me Me       CH.sub.2                                   4-Br                                                                               5-Cl                                                                              Ph   H  CO.sub.2 Me Me       CH.sub.2                                   __________________________________________________________________________

                  TABLE 14                                                         ______________________________________                                          ##STR25##                                                                     R.sub.1     R.sub.2  R.sub.3    R.sub.4                                                                             A                                         ______________________________________                                         4-CF.sub.3  5-Cl     Ph         H    CH.sub.2                                  4-Cl        5-Cl     Ph         H    CH.sub.2                                  4-Br        5-Cl     Ph         H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     Ph         H    CH.sub.2                                  4-CF.sub.3  5-Cl     4-ClPh     H    CH.sub.2                                  4-Cl        5-Cl     4-ClPh     H    CH.sub.2                                  4-Br        5-Cl     4-ClPh     H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     4-ClPh     H    CH.sub.2                                  4-CF.sub.3  5-Cl     4-FPh      H    CH.sub.2                                  4-Cl        5-Cl     4-FPh      H    CH.sub.2                                  4-Br        5-Cl     4-FPh      H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     4-FPh      H    CH.sub.2                                  4-CF.sub.3  5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2                                  4-Cl        5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2                                  4-Br        5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2                                  4-CF.sub.3  5-F      Ph         H    CH.sub.2                                  4-Cl        5-F      Ph         H    CH.sub.2                                  4-Br        5-F      Ph         H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      Ph         H    CH.sub.2                                  4-CF.sub.3  5-F      4-FPh      H    CH.sub.2                                  4-Cl        5-F      4-FPh      H    CH.sub.2                                  4-Br        5-F      4-FPh      H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      4-FPh      H    CH.sub.2                                  4-CF.sub.3  5-F      4-ClPh     H    CH.sub.2                                  4-Cl        5-F      4-ClPh     H    CH.sub.2                                  4-Br        5-F      4-ClPh     H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      4-ClPh     H    CH.sub.2                                  4-CF.sub.3  5-F      4-OMePh    H    CH.sub.2                                  4-Cl        5-F      4-OMePh    H    CH.sub.2                                  4-Br        5-F      4-OMePh    H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      4-OMePh    H    CH.sub.2                                  4-CF.sub.3  5-Cl     Ph         Me   CH.sub.2                                  4-Cl        5-Cl     Ph         Me   CH.sub.2                                  4-Br        5-Cl     Ph         Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     Ph         Me   CH.sub.2                                  4-CF.sub.3  5-Cl     5-Cl       Me   CH.sub.2                                  4-Cl        5-Cl     5-Cl       Me   CH.sub.2                                  4-Br        5-Cl     5-Cl       Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     5-Cl       Me   CH.sub.2                                  4-CF.sub.3  5-F      Ph         Me   CH.sub.2                                  4-Cl        5-F      Ph         Me   CH.sub.2                                  4-Br        5-F      Ph         Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      Ph         Me   CH.sub.2                                  4-CF.sub.3  5-F      5-Cl       Me   CH.sub.2                                  4-Cl        5-F      5-Cl       Me   CH.sub.2                                  4-Br        5-F      5-Cl       Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              5-F      5-Cl       Me   CH.sub.2                                  4-CF.sub.3  5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2                                  4-Cl        5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2                                  4-Br        5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2                                  4-CF.sub.3  5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-Cl        5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-Br        5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-CF.sub.3  4-F      CO.sub.2 Me                                                                               H    CH.sub.2                                  4-Cl        4-F      CO.sub.2 Me                                                                               H    CH.sub.2                                  4-Br        4-F      CO.sub.2 Me                                                                               H    CH.sub.2                                  4-OCF.sub.2 H                                                                              4-F      CO.sub.2 Me                                                                               H    CH.sub.2                                  4-CF.sub.3  4-F      CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-Cl        4-F      CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-Br        4-F      CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-OCF.sub.2 H                                                                              4-F      CO.sub.2 Me                                                                               Me   CH.sub.2                                  4-OCF.sub.3 5-Cl     4-ClPh     H    CH.sub.2                                  4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     4-ClPh     H    CH.sub.2                                  3-Cl,4-CF.sub.3                                                                            5-Cl     4-ClPh     H    CH.sub.2                                  3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     4-ClPh     H    CH.sub.2                                  3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     4-ClPh     H    CH.sub.2                                  4-CN        5-Cl     4-ClPh     H    CH.sub.2                                  4-NO.sub.2  5-Cl     4-ClPh     H    CH.sub.2                                  4-F         5-Cl     4-ClPh     H    CH.sub.2                                  3,4-di-Cl   5-Cl     4-ClPh     H    CH.sub.2                                  4-CO.sub.2 Me                                                                              5-Cl     4-ClPh     H    CH.sub.2                                  4-SCF.sub.2 H                                                                              5-Cl     4-ClPh     H    CH.sub.2                                  4-SCF.sub.2 CF.sub.2 H                                                                     5-Cl     4-ClPh     H    CH.sub.2                                  4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     4-ClPh     H    CH.sub.2                                  4-OCF.sub.3 5-Cl     Ph         H    CH.sub.2                                  4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     Ph         H    CH.sub.2                                  3-Cl,4-CF.sub.3                                                                            5-Cl     Ph         H    CH.sub.2                                  3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     Ph         H    CH.sub.2                                  3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     Ph         H    CH.sub.2                                  4-CN        5-Cl     Ph         H    CH.sub.2                                  4-NO.sub.2  5-Cl     Ph         H    CH.sub.2                                  4-F         5-Cl     Ph         H    CH.sub.2                                  3,4-di-Cl   5-Cl     Ph         H    CH.sub.2                                  4-CO.sub.2 Me                                                                              5-Cl     Ph         H    CH.sub.2                                  4-SCF.sub.2 H                                                                              5-Cl     Ph         H    CH.sub.2                                  4-SCF.sub.2 CF.sub.2 H                                                                     5-Cl     Ph         H    CH.sub.2                                  4-OCH.sub.2 CF.sub.3                                                                       5-Cl     Ph         H    CH.sub.2                                  4-CF.sub.3  5-Cl     Ph         Me   O                                         4-Cl        5-Cl     Ph         Me   O                                         4-Br        5-Cl     Ph         Me   O                                         4-OCF.sub.2 H                                                                              5-Cl     Ph         Me   O                                         4-CF.sub.3  5-Cl     4-ClPh     Me   O                                         4-Cl        5-Cl     4-ClPh     Me   O                                         4-Br        5-Cl     4-ClPh     Me   O                                         4-OCF.sub.2 H                                                                              5-Cl     4-ClPh     Me   O                                         4-CF.sub.3  5-F      Ph         Me   O                                         4-Cl        5-F      Ph         Me   O                                         4-Br        5-F      Ph         Me   O                                         4-OCF.sub.2 H                                                                              5-F      Ph         Me   O                                         4-CF.sub.3  5-F      4-ClPh     Me   O                                         4-Cl        5-F      4-ClPh     Me   O                                         4-Br        5-F      4-ClPh     Me   O                                         4-OCF.sub.2 H                                                                              5-F      4-ClPh     Me   O                                         4-CF.sub.3  5-F      Me         allyl                                                                               O                                         4-OCF.sub.3 5-F      Me         allyl                                                                               O                                         4-CF.sub.3  5-Cl     Me         allyl                                                                               O                                         4-OCF.sub.3 5-Cl     Me         allyl                                                                               O                                         4-CF.sub.3  5-CF.sub.3                                                                              Me         allyl                                                                               O                                         4-OCF.sub.3 5-CF.sub.3                                                                              Me         allyl                                                                               O                                         4-CF.sub.3  5-F      CH.sub.2 Ph                                                                               Me   O                                         4-OCF.sub.3 5-F      CH.sub.2 Ph                                                                               Me   O                                         4-CF.sub.3  5-Cl     CH.sub.2 Ph                                                                               Me   O                                         4-OCF.sub.3 5-Cl     CH.sub.2 Ph                                                                               Me   O                                         4-CF.sub.3  5-F      Me         H    O                                         4-OCF.sub.3 5-F      Me         H    O                                         4-CF.sub.3  5-Cl     Me         H    O                                         4-OCF.sub.3 5-Cl     Me         H    O                                         4-CF.sub.3  5-F      i-Pr       H    O                                         4-OCF.sub.3 5-F      i-Pr       H    O                                         4-CF.sub.3  5-Cl     i-Pr       H    O                                         4-OCF.sub.3 5-Cl     i-Pr       H    O                                         4-CF.sub.3  5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-Cl        5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-Br        5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-Cl        5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-Br        5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     4-FPh      H    CH.sub.2 CH.sub.2                         4-Cl        5-Cl     4-FPh      H    CH.sub.2 CH.sub.2                         4-Br        5-Cl     4-FPh      H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     4-FPh      H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2 CH.sub.2                         4-Cl        5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2 CH.sub.2                         4-Br        5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     4-NO.sub.2 Ph                                                                             H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-F      Ph         H    CH.sub.2 CH.sub.2                         4-Cl        5-F      Ph         H    CH.sub. 2 CH.sub.2                        4-Br        5-F      Ph         H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      Ph         H    CH.sub.2 CH.sub.2                         4-CF3       5-F      4-FPh      H    CH.sub.2 CH.sub.2                         4-Cl        5-F      4-FPh      H    CH.sub.2 CH.sub.2                         4-Br        5-F      4-FPh      H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      4-FPh      H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-F      4-ClPh     H    CH.sub.2 CH.sub.2                         4-Cl        5-F      4-ClPh     H    CH.sub.2 CH.sub.2                         4-Br        5-F      4-ClPh     H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      4-ClPh     H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-F      4-OMe      H    CH.sub.2 CH.sub.2                         4-Cl        5-F      4-OMe      H    CH.sub.2 CH.sub.2                         4-Br        5-F      4-OMe      H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      4-OMe      H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     Ph         Me   CH.sub.2 CH.sub.2                         4-Cl        5-Cl     Ph         Me   CH.sub.2 CH.sub.2                         4-Br        5-Cl     Ph         Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     Ph         Me   CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     4-ClPh     Me   CH.sub.2 CH.sub.2                         4-Cl        5-Cl     4-ClPh     Me   CH.sub.2 CH.sub.2                         4-Br        5-Cl     4-ClPh     Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     4-ClPh     Me   CH.sub.2 CH.sub.2                         4-CF.sub.3  5-F      Ph         Me   CH.sub.2 CH.sub.2                         4-Cl        5-F      Ph         Me   CH.sub.2 CH.sub.2                         4-Br        5-F      Ph         Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      Ph         Me   CH.sub.2 CH.sub.2                         4-CF.sub.3  5-F      4-ClPh     Me   CH.sub.2 CH.sub.2                         4-Cl        5-F      4-ClPh     Me   CH.sub.2 CH.sub.2                         4-Br        5-F      4-ClPh     Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-F      4-ClPh     Me   CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-Cl        5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-Br        5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-CF.sub.3  5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-Cl        5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-Br        5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              5-Cl     CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-CF.sub.3  4-F      CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-Cl        4-F      CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-Br        4-F      CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              4-F      CO.sub.2 Me                                                                               H    CH.sub.2 CH.sub.2                         4-CF.sub.3  4-F      CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-Cl        4-F      CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-Br        4-F      CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-OCF.sub.2 H                                                                              4-F      CO.sub.2 Me                                                                               Me   CH.sub.2 CH.sub.2                         4-OCF.sub.3 5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         3-Cl,4-CF.sub.3                                                                            5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-CN        5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-NO.sub.2  5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-F         5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         3,4-di-Cl   5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-CO.sub.2 Me                                                                              5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-SCF.sub.2 H                                                                              5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-SCF.sub.2 CF.sub.2 H                                                                     5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-OCH.sub.2 CF.sub.3                                                                       5-Cl     4-ClPh     H    CH.sub.2 CH.sub.2                         4-OCF.sub.3 5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-OCF.sub.2 CF.sub.2 H                                                                     5-Cl     Ph         H    CH.sub.2 CH.sub.2                         3-Cl,4-CF.sub.3                                                                            5-Cl     Ph         H    CH.sub.2 CH.sub.2                         3,4-CH.sub.2 C(Me).sub.2 O                                                                 5-Cl     Ph         H    CH.sub.2 CH.sub.2                         3,4-CF.sub.2 CF.sub.2 O                                                                    5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-CN        5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-NO.sub.2  5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-F         5-Cl     Ph         H    CH.sub.2 CH.sub.2                         3,4-di-Cl   5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-CO.sub.2 Me                                                                              5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-SCF.sub.2 H                                                                              5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-SCF.sub.2 CF.sub.2 H                                                                     5-Cl     Ph         H    CH.sub.2 CH.sub.2                         4-OCH.sub.2 CF.sub.3                                                                       5-Cl     Ph         H    CH.sub.2 CH.sub.2                         ______________________________________                                    

                  TABLE 15                                                         ______________________________________                                          ##STR26##                                                                     Q      R.sub.1  R.sub.2   R.sub.3 R.sub.4                                                                              A                                      ______________________________________                                         Q-2    CF.sub.3 H         H       H     CH.sub.2                               Q-2    OCF.sub.3                                                                               H         H       H     CH.sub.2                               Q-2    CF.sub.3 H         Me      H     CH.sub.2                               Q-2    OCF.sub.3                                                                               H         Me      H     CH.sub.2                               Q-2    CF.sub.3 H         4-FPh   H     CH.sub.2                               Q-2    OCF.sub.3                                                                               H         4-FPh   H     CH.sub.2                               Q-2    CF.sub.3 H         4-ClPh  H     CH.sub.2                               Q-2    OCF.sub.3                                                                               H         4-ClPh  H     CH.sub.2                               Q-2    CF.sub.3 5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-2    CF.sub.3 5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-2    CF.sub.3 5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-2    CF.sub.3 5-Cl      Me      H     CH.sub.2                               Q-2    OCF.sub.3                                                                               5-Cl      Me      H     CH.sub.2                               Q-2    CF.sub.3 5-Cl      4-FPh   H     CH.sub.2                               Q-2    OCF.sub.3                                                                               5-Cl      4-FPh   H     CH.sub.2                               Q-2    CF.sub.3 H         H       H     O                                      Q-2    OCF.sub.3                                                                               H         H       H     O                                      Q-2    CF.sub.3 H         Me      H     O                                      Q-2    OCF.sub.3                                                                               H         Me      H     O                                      Q-2    CF.sub.3 H         4-FPh   Me    O                                      Q-2    OCF.sub.3                                                                               H         4-FPh   Me    O                                      Q-2    CF.sub.3 H         4-ClPh  Me    O                                      Q-2    OCF.sub.3                                                                               H         4-ClPh  Me    O                                      Q-2    CF.sub.3 H         i-Pr    H     O                                      Q-2    OCF.sub.3                                                                               H         i-Pr    H     O                                      Q-2    CF.sub.3 5-CF.sub.3                                                                               H       H     O                                      Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               H       H     O                                      Q-2    CF.sub.3 5-CF.sub.3                                                                               Me      H     O                                      Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     O                                      Q-2    CF.sub.3 5-CF.sub.3                                                                               i-Pr    H     O                                      Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               i-Pr    H     O                                      Q-2    CF.sub.3 5-CF.sub.3                                                                               4-FPh   Me    O                                      Q-2    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-FPh   Me    O                                      Q-3    CF.sub.3 H         H       H     CH.sub.2                               Q-3    OCF.sub.3                                                                               H         H       H     CH.sub.2                               Q-3    CF.sub.3 H         Me      H     CH.sub.2                               Q-3    OCF.sub.3                                                                               H         Me      H     CH.sub.2                               Q-3    CF.sub.3 H         4-FPh   H     CH.sub.2                               Q-3    OCF.sub.3                                                                               H         4-FPh   H     CH.sub.2                               Q-3    CF.sub.3 H         4-ClPh  H     CH.sub.2                               Q-3    OCF.sub.3                                                                               H         4-ClPh  H     CH.sub.2                               Q-3    CF.sub.3 4-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-3    CF.sub.3 4-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-3    CF.sub.3 4-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-3    CF.sub.3 4-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-3    CF.sub.3 4-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-3    CF.sub.3 H         H       H     O                                      Q-3    OCF.sub.3                                                                               H         H       H     O                                      Q-3    CF.sub.3 H         Me      H     O                                      Q-3    OCF.sub.3                                                                               H         Me      H     O                                      Q-3    CF.sub.3 H         4-FPh   Me    O                                      Q-3    OCF.sub.3                                                                               H         4-FPh   Me    O                                      Q-3    CF.sub.3 H         4-ClPh  Me    O                                      Q-3    OCF.sub.3                                                                               H         4-ClPh  Me    O                                      Q-3    CF.sub.3 H         i-Pr    H     O                                      Q-3    OCF.sub.3                                                                               H         i-Pr    H     O                                      Q-3    CF.sub.3 4-CF.sub.3                                                                               H       H     O                                      Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               H       H     O                                      Q-3    CF.sub.3 4-CF.sub.3                                                                               Me      H     O                                      Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               Me      H     O                                      Q-3    CF.sub.3 4-CF.sub.3                                                                               i-Pr    H     O                                      Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               i-Pr    H     O                                      Q-3    CF.sub.3 4-CF.sub.3                                                                               4-FPh   Me    O                                      Q-3    OCF.sub.3                                                                               4-CF.sub.3                                                                               4-FPh   Me    O                                      Q-4    CF.sub.3 H         H       H     CH.sub.2                               Q-4    OCF.sub.3                                                                               H         H       H     CH.sub.2                               Q-4    CF.sub.3 H         Me      H     CH.sub.2                               Q-4    OCF.sub.3                                                                               H         Me      H     CH.sub.2                               Q-4    CF.sub.3 H         4-FPh   H     CH.sub.2                               Q-4    OCF.sub.3                                                                               H         4-FPh   H     CH.sub.2                               Q-4    CF.sub.3 H         4-ClPh  H     CH.sub.2                               Q-4    OCF.sub.3                                                                               H         4-ClPh  H     CH.sub.2                               Q-4    CF.sub.3 5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-4    CF.sub.3 5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-4    CF.sub.3 5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-4    CF.sub.3 4-F       Me      H     CH.sub.2                               Q-4    OCF.sub.3                                                                               4-F       Me      H     CH.sub.2                               Q-4    CF.sub.3 4-F       4-FPh   H     CH.sub. 2                              Q-4    OCF.sub.3                                                                               4-F       4-FPh   H     CH.sub.2                               Q-4    CF.sub.3 H         H       H     O                                      Q-4    OCF.sub.3                                                                               H         H       H     O                                      Q-4    CF.sub.3 H         Me      H     O                                      Q-4    OCF.sub.3                                                                               H         Me      H     O                                      Q-4    CF.sub.3 H         4-FPh   Me    O                                      Q-4    OCF.sub.3                                                                               H         4-FPh   Me    O                                      Q-4    CF.sub.3 H         4-ClPh  Me    O                                      Q-4    OCF.sub.3                                                                               H         4-ClPh  Me    O                                      Q-4    CF.sub.3 H         i-Pr    H     O                                      Q-4    OCF.sub.3                                                                               H         i-Pr    H     O                                      Q-4    CF.sub.3 5-CF.sub.3                                                                               H       H     O                                      Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               H       H     O                                      Q-4    CF.sub.3 5-CF.sub.3                                                                               Me      H     O                                      Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     O                                      Q-4    CF.sub.3 5-CF.sub.3                                                                               i-Pr    H     O                                      Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               i-Pr    H     O                                      Q-4    CF.sub.3 5-CF.sub.3                                                                               4-FPh   H     O                                      Q-4    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-FPh   H     O                                      Q-5    CF.sub.3 H         H       H     CH.sub.2                               Q-5    OCF.sub.3                                                                               H         H       H     CH.sub.2                               Q-5    CF.sub.3 H         Me      H     CH.sub.2                               Q-5    OCF.sub.3                                                                               H         Me      H     CH.sub.2                               Q-5    CF.sub.3 H         4-FPh   H     CH.sub.2                               Q-5    OCF.sub.3                                                                               H         4-FPh   H     CH.sub.2                               Q-5    CF.sub.3 H         4-ClPh  H     CH.sub.2                               Q-5    OCF.sub.3                                                                               H         4-ClPh  H     CH.sub.2                               Q-5    CF.sub.3 5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     CH.sub.2                               Q-5    CF.sub.3 5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-FPh   H     CH.sub.2                               Q-5    CF.sub.3 5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-ClPh  H     CH.sub.2                               Q-5    CF.sub.3 4-F       Me      H     CH.sub.2                               Q-5    OCF.sub.3                                                                               4-F       Me      H     CH.sub.2                               Q-5    CF.sub.3 4-F       4-FPh   H     CH.sub.2                               Q-5    OCF.sub.3                                                                               4-F       4-FPh   H     CH.sub.2                               Q-5    CF.sub.3 5-CF.sub.3                                                                               H       H     O                                      Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               H       H     O                                      Q-5    CF.sub.3 5-CF.sub.3                                                                               Me      H     O                                      Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               Me      H     O                                      Q-5    CF.sub.3 5-CF.sub.3                                                                               4-FPh   Me    O                                      Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-.sub.3 FPh                                                                           Me    O                                      Q-5    CF.sub.3 5-CF.sub.3                                                                               4-ClPh  Me    O                                      Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               4-ClPh  Me    O                                      Q-5    CF.sub.3 5-CF.sub.3                                                                               i-Pr    H     O                                      Q-5    OCF.sub.3                                                                               5-CF.sub.3                                                                               i-Pr    H     O                                      Q-5    CF.sub.3 5-Cl      H       H     O                                      Q-5    OCF.sub.3                                                                               5-Cl      H       H     O                                      Q-5    CF.sub.3 5-Cl      Me      H     O                                      Q-5    OCF.sub.3                                                                               5-Cl      Me      H     O                                      Q-5    CF.sub.3 5-Cl      i-Pr    H     O                                      Q-5    OCF.sub.3                                                                               5-Cl      i-Pr    H     O                                      Q-5    CF.sub.3 5-Cl      4-FPh   Me    O                                      Q-5    OCF.sub.3                                                                               5-Cl      4-FPh   Me    O                                      ______________________________________                                    

                  TABLE 16                                                         ______________________________________                                          ##STR27##                                                                     (V = S)                                                                        Q       R.sub.1   R.sub.2 R.sub.3  R.sub.4                                                                              A                                     ______________________________________                                         Q-6     CF.sub.3  H       H        H     CH.sub.2                              Q-6     OCF.sub.3 H       H        H     CH.sub.2                              Q-6     CF.sub.3  H       Me       H     CH.sub.2                              Q-6     OCF.sub.3 H       Me       H     CH.sub.2                              Q-6     CF.sub.3  H       4-FPh    H     CH.sub.2                              Q-6     OCF.sub.3 H       4-FPh    H     CH.sub.2                              Q-6     CF.sub.3  H       4-ClPh   H     CH.sub.2                              Q-6     OCF.sub.3 H       4-ClPh   H     CH.sub.2                              Q-6     CF.sub.3  5-Cl    Me       H     CH.sub.2                              Q-6     OCF.sub.3 5-Cl    Me       H     CH.sub.2                              Q-6     CF.sub.3  5-Cl    4-FPh    H     CH.sub.2                              Q-6     OCF.sub.3 5-Cl    4-FPh    H     CH.sub.2                              Q-6     CF.sub.3  5-Cl    4-ClPh   H     CH.sub.2                              Q-6     OCF.sub.3 5-Cl    4-ClPh   H     CH.sub.2                              Q-6     CF.sub.3  5-F     Me       H     CH.sub.2                              Q-6     OCF.sub.3 5-F     Me       H     CH.sub.2                              Q-6     CF.sub.3  5-F     4-FPh    H     CH.sub.2                              Q-6     OCF.sub.3 5-F     4-F Ph   H     CH.sub.2                              Q-6     CF.sub.3  H       H        H     O                                     Q-6     OCF.sub.3 H       H        H     O                                     Q-6     CF.sub.3  H       Me       H     O                                     Q-6     OCF.sub.3 H       Me       H     O                                     Q-6     CF.sub.3  H       4-FPh    Me    O                                     Q-6     OCF.sub.3 H       4-.sub.3 FPh                                                                            Me    O                                     Q-6     CF.sub.3  H       4-ClPh   Me    O                                     Q-6     OCF.sub.3 H       4-ClPh   Me    O                                     Q-6     CF.sub.3  H       i-Pr     H     O                                     Q-6     OCF.sub.3 H       i-Pr     H     O                                     Q-6     CF.sub.3  5-Cl    H        H     O                                     Q-6     OCF.sub.3 5-Cl    H        H     O                                     Q-6     CF.sub.3  5-Cl    Me       H     O                                     Q-6     OCF.sub.3 5-Cl    Me       H     O                                     Q-6     CF.sub.3  5-Cl    i-Pr     H     O                                     Q-6     OCF.sub.3 5-Cl    i-Pr     H     O                                     Q-6     CF.sub.3  5-Cl    4-FPh    Me    O                                     Q-6     OCF.sub.3 5-Cl    4-FPh    Me    O                                     Q-7     CF.sub.3  H       H        H     CH.sub.2                              Q-7     OCF.sub.3 H       H        H     CH.sub.2                              Q-7     CF.sub.3  H       Me       H     CH.sub.2                              Q-7     OCF.sub.3 H       Me       H     CH.sub.2                              Q-7     CF.sub.3  H       4-FPh    H     CH.sub.2                              Q-7     OCF.sub.3 H       4-FPh    H     CH.sub.2                              Q-7     CF.sub.3  H       4-ClPh   H     CH.sub.2                              Q-7     OCF.sub.3 H       4-ClPh   H     CH.sub.2                              Q-7     CF.sub.3  4-Cl    Me       H     CH.sub.2                              Q-7     OCF.sub.3 4-Cl    Me       H     CH.sub.2                              Q-7     CF.sub.3  4-Cl    4-FPh    H     CH.sub.2                              Q-7     OCF.sub.3 4-Cl    4-FPh    H     CH.sub.2                              Q-7     CF.sub.3  4-Cl    4-ClPh   H     CH.sub.2                              Q-7     OCF.sub.3 4-Cl    4-ClPh   H     CH.sub.2                              Q-7     CF.sub.3  4-F     Me       H     CH.sub.2                              Q-7     OCF.sub.3 4-F     Me       H     CH.sub.2                              Q-7     CF.sub.3  4-F     4-FPh    H     CH.sub.2                              Q-7     OCF.sub.3 4-F     4-FPh    H     CH.sub.2                              Q-7     CF.sub.3  H       H        H     O                                     Q-7     OCF.sub.3 H       H        H     O                                     Q-7     CF.sub.3  H       Me       H     O                                     Q-7     OCF.sub.3 H       Me       H     O                                     Q-7     CF.sub.3  H       4-FPh    Me    O                                     Q-7     OCF.sub.3 H       4-.sub.3 FPh                                                                            Me    O                                     Q-7     CF.sub.3  H       4-ClPh   Me    O                                     Q-7     OCF.sub.3 H       4-ClPh   Me    O                                     Q-7     CF.sub.3  H       i-Pr     H     O                                     Q-7     OCF.sub.3 H       i-Pr     H     O                                     Q-7     CF.sub.3  4-F     H        H     O                                     Q-7     OCF.sub.3 4-F     H        H     O                                     Q-7     CF.sub.3  4-F     Me       H     O                                     Q-7     OCF.sub.3 4-F     Me       H     O                                     Q-7     CF.sub.3  4-F     i-Pr     H     O                                     Q-7     OCF.sub.3 4-F     i-Pr     H     O                                     Q-7     CF.sub.3  4-F     4-FPh    Me    O                                     Q-7     OCF.sub.3 4-F     4-FPh    Me    O                                     Q-8     CF.sub.3  H       H        H     CH.sub.2                              Q-8     OCF.sub.3 H       H        H     CH.sub.2                              Q-8     CF.sub.3  H       Me       H     CH.sub.2                              Q-8     OCF.sub.3 H       Me       H     CH.sub.2                              Q-8     CF.sub.3  H       4-FPh    H     CH.sub.2                              Q-8     OCF.sub.3 H       4-FPh    H     CH.sub.2                              Q-8     CF.sub.3  H       4-ClPh   H     CH.sub.2                              Q-8     OCF.sub.3 H       4-ClPh   H     CH.sub.2                              Q-8     CF.sub.3  4-F     Me       H     CH.sub.2                              Q-8     OCF.sub.3 4-F     Me       H     CH.sub.2                              Q-8     CF.sub.3  4-F     4-FPh    H     CH.sub.2                              Q-8     OCF.sub.3 4-F     4-FPh    H     CH.sub.2                              Q-8     CF.sub.3  4-F     4-ClPh   H     CH.sub.2                              Q-8     OCF.sub.3 4-F     4-ClPh   H     CH.sub.2                              Q-8     CF.sub.3  5-Cl    Me       H     CH.sub.2                              Q-8     OCF.sub.3 5-Cl    Me       H     CH.sub.2                              Q-8     CF.sub.3  5-Cl    4-FPh    H     CH.sub.2                              Q-8     OCF.sub.3 5-Cl    4-FPh    H     CH.sub.2                              Q-8     CF.sub.3  4-F     H        H     O                                     Q-8     OCF.sub.3 4-F     H        H     O                                     Q-8     CF.sub.3  4-F     Me       H     O                                     Q-8     OCF.sub.3 4-F     Me       H     O                                     Q-8     CF.sub.3  4-F     4-FPh    Me    O                                     Q-8     OCF.sub.3 4-F     4-.sub.3 FPh                                                                            Me    O                                     Q-8     CF.sub.3  4-F     4-ClPh   Me    O                                     Q-8     OCF.sub.3 4-F     4-ClPh   Me    O                                     Q-8     CF.sub.3  4-F     i-Pr     H     O                                     Q-8     OCF.sub.3 4-F     i-Pr     H     O                                     Q-8     CF.sub.3  5-Cl    H        H     O                                     Q-8     OCF.sub.3 5-Cl    H        H     O                                     Q-8     CF.sub.3  5-Cl    Me       H     O                                     Q-8     OCF.sub.3 5-Cl    Me       H     O                                     Q-8     CF.sub.3  5-Cl    i-Pr     H     O                                     Q-8     OCF.sub.3 5-Cl    i-Pr     H     O                                     Q-8     CF.sub.3  5-Cl    4-FPh    Me    O                                     Q-8     OCF.sub.3 5-Cl    4-FPh    Me    O                                     ______________________________________                                    

ARTHROPODICIDAL FORMULATION AND USE

The compounds of this invention will generally be used in formulation with a carrier comprising a liquid or solid diluent or an organic solvent. Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, baits, wettable powders, emulsifiable concentrates, dry flowables and the like. Many of these can be applied directly. Sprayable formulations can be extended in suitable media and used at spray volumes of from about one to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, contain about 1% to 99% by weight of active ingredient(s): and at least one of a) about 0.1% to 20% surfactant(s) and b) about 5% to 99% solid or liquid diluent(s). More specifically, they will contain these ingredients in the following approximate proportions:

    ______________________________________                                                     Percent by Weight                                                              Active                                                                         Ingredient                                                                             Diluent(s)                                                                               Surfactant(s)                                    ______________________________________                                         Wettable Powders                                                                             25-90     0-74      1-10                                         Oil Suspensions,                                                                              1-50     40-95     0-35                                         Emulsions, Solutions,                                                          (including Emulsifiable                                                        Concentrates)                                                                  Dusts          1-25     70-99     0-5                                          Granules, Baits                                                                              0.01-95   5-99      0-15                                         and Pellets                                                                    High Strength 90-99     0-10      0-2                                          Compositions                                                                   ______________________________________                                    

Lower or higher levels of active ingredient can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books, Caldwell, N.J. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide," 2nd Ed., Interscience, New York, 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are Preferably stable against phase separation at 0° C. "McCutcheon's Detergents and Emulsifiers Annual", Allured Publ. Corp., Ridgewood, N.J., as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publ. Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foam, caking, corrosion, microbiological growth, etc. Preferably, ingredients should be approved by the U.S. Environmental Protection Agency for the use intended.

The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, U.S. Pat. No. 3,060,084). Granules and pellets can be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See Browning, "Agglomeration", Chemical Engineering, Dec. 4, 1967, pages 147 and following, and "Perry's Chemical Engineer's Handbook", 4th Ed., McGraw-Hill, New York, 1963, pages 8 to 59 and following.

EXAMPLE A Emulsifiable Concentrate

    ______________________________________                                         2-(5-chloro-2,3-dihydro-2-phenyl-1H-inden-1-ylidene)-                                                     20%                                                 N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide                              blend of oil soluble sulfonates                                                                           10%                                                 and polyoxyethylene ethers                                                     isophorone                 70%                                                 ______________________________________                                    

The ingredients are combined and stirred with gentle warming to speed solution. A fine screen filter is included in packaging operation to insure the absence of any extraneous undissolved material in the product.

EXAMPLE B Wettable Powder

    ______________________________________                                         2-(5-chloro-2,3-dihydro-2-phenyl-1H-inden-1-ylidene)-                                                      30%                                                N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide                              sodium alkylnaphthalenesulfonate                                                                           2%                                                 sodium ligninsulfonate      2%                                                 synthetic amorphous silica  3%                                                 kaolinite                   63%                                                ______________________________________                                    

The active ingredient is mixed with the inert materials in a blender. After grinding in a hammermill, the material is re-blended and sifted through a 50 mesh screen.

EXAMPLE C Dust

    ______________________________________                                         Wettable powder of Example B                                                                         10%                                                      pyrophyllite (powder) 90%                                                      ______________________________________                                    

The wettable powder and the pyrophyllite diluent are thoroughly blended and then packaged. The product is suitable for use as a dust.

EXAMPLE D Granule

    ______________________________________                                         2-[5-chloro-2-(4-chlorophenyl)-2,3-dihydro-1H-inden-1-y                                                     10%                                               lidene]-N-[4-(trifluoromethyl)phenyl]hydrazine-                                carboxamide                                                                    attapulgite granules (low volative                                                                          90%                                               matter, 0.71/0.30 mm; U.S.S. No.                                               25-50 sieves)                                                                  ______________________________________                                    

The active ingredient is dissolved in a volatile solvent such as acetone and sprayed upon dedusted and pre-warmed attapulgite granules in a double cone blender. The acetone is then driven off by heating. The granules are then allowed to cool and are packaged.

EXAMPLE E Granule

    ______________________________________                                         Wettable powder of Example B                                                                         15%                                                      gypsum                69%                                                      potassium sulfate     16%                                                      ______________________________________                                    

The ingredients are blended in a rotating mixer and water sprayed on to accomplish granulation. When most of the material has reached the desired range of 0.1 to 0.42 mm (U.S.S. No. 18 to 40 sieves), the granules are removed, dried, and screened. Oversize material is crushed to produce additional material in the desired range. These granules contain 4.5% active ingredient.

EXAMPLE F Solution

    ______________________________________                                         2-(5-chloro-2,3-dihydro-2-phenyl-1H-inden-1-ylidene)-                                                     25%                                                 N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide                              N-methyl-pyrrolidone       75%                                                 ______________________________________                                    

The ingredients are combined and stirred to produce a solution suitable for direct, low volume application.

EXAMPLE G Aqueous Suspension

    ______________________________________                                         2-(5-chloro-2,3-dihydro-2-phenyl-1H-inden-1-ylidene)-                                                      40%                                                N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide                              polyacrylic acid thickener  0.3%                                               dodecyclophenol polyethylene glycol ether                                                                  0.5%                                               disodium phosphate          1.0%                                               monosodium phosphate        0.5%                                               polyvinyl alcohol           1.0%                                               water                       56.7%                                              ______________________________________                                    

The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size.

EXAMPLE H Oil Suspension

    ______________________________________                                         2-[5-chloro-2-(4-chlorophenyl)-2,3-dihydro-1H-inden-1-y                                                     35.0%                                             lidene]-N-[4-(trifluoromethyl)phenyl]hydrazine-                                carboxamide                                                                    blend of polyalcohol carboxylic                                                                              6.0%                                             esters and oil soluble petroleum                                               sulfonates                                                                     xylene range solvent         59.0%                                             ______________________________________                                    

The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water.

EXAMPLE I Bait Granules

    ______________________________________                                         2-(5-chloro-2,3-dihydro-2-phenyl-1H-inden-1-ylidene)-                                                     3.0%                                                N-[4-(trifluoromethyl)phenyl]hydrazinecarboxamide                              blend of polyethoxylated nonyl-                                                                           9.0%                                                phenols and sodium dodecyl-                                                    benzene sulfonates                                                             ground up corn cobs        88.0%                                               ______________________________________                                    

The active ingredient and surfactant blend are dissolved in a suitable solvent such as acetone and sprayed onto the ground corn cobs. The granules are then dried and packaged. Compounds of Formula I can also be mixed with one or more other insecticides, fungicides, nematocides, bactericides, acaricides, or other biologically active compounds to form a multi-component pesticide giving an even broader spectrum of effective agricultural protection. Examples of other agricultural protectants with which compounds of the present invention can be mixed or formulated are:

Insecticides

3-hydroxy-N-methylcrotonamide(dimethylphosphate)ester (monocrotophos)

methylcarbamic acid, ester with 2,3-dihydro-2,2-dimethyl-7-benzofuranol (carbofuran)

O-[2,4,5-trichloro-α-(chloromethyl)benzyl]phosphoric acid, O',O'-dimethyl ester (tetrachlorvinphos)

2-mercaptosuccinic acid, diethyl ester, S-ester with thionophosphoric acid, dimethyl ester (malathion)

phosphorothioic acid, O,O-dimethyl, O-p-nitrophenyl ester (methyl parathion)

methylcarbamic acid, ester with α-naphthol (carbaryl)

methyl O-(methylcarbamoyl)thiolacetohydroxamate (methomyl)

N'-(4-chloro-o-tolyl)-N,N-dimethylformamidine (chlordimeform)

O,O-diethyl-O-(2-isopropyl-4-methyl-6-pyrimidylphosphorothioate (diazinon)

octachlorocamphene (toxaphene)

O-ethyl O-p-nitrophenyl phenylphosphonothioate (EPN)

(S)-a-cyano-m-phenoxybenzyl(1R,3R)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate (deltamethrin)

Methyl-N ,N -dimethyl-N-[(methylcarbamoyl)oxy]-1-thioox amimidate (oxamyl)

cyano(3-phenoxyphenyl)-methyl-4-chloro-a-(1-methylethyl)benzeneacetate (fenvalerate)

(3-phenoxyphenyl)methyl(+)-cis,trans-3-(2,2-dichloro ethenyl)-2,2-dimethylcyclopropanecarboxylate (permethrin)

a-cyano-3-phenoxybenzyl 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylate (cypermethrin)

O-ethyl-S-(p-chlorophenyl)ethylphosphonodithioate (profenofos)

phosphorothiolothionic acid,

O-ethyl-O-[4-(methylthio)-phenyl]-S-n-propyl ester (sulprofos).

Additional insecticides are listed hereafter by their common names: triflumuron, diflubenzuron, methoprene, buprofezin, thiodicarb, acephate, azinphosmethyl, chlorpyrifos, dimethoate, fonophos, isofenphos, methidathion, methamidiphos, monocrotphos, phosmet, phosphamidon, phosalone, pirimicarb, phorate, profenofos, terbufos, trichlorfon, methoxychlor, bifenthrin, biphenate, cyfluthrin, fenpropathrin, fluvalinate, flucythrinate, tralomethrin, metaldehyde and rotenone.

FUNGICIDES

methyl 2-benzimidazolecarbamate (carbendazim)

tetramethylthiuram disulfide (thiuram)

n-dodecylguanidine acetate (dodine)

manganese ethylenebisdithiocarbamate (maneb)

1,4-dichloro-2,5-dimethoxybenzene (chloroneb)

methyl 1-(butylcarbamoly)-2-benzimidazolecarbamate (benomyl)

1-[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-ylmethyl]-1H-1,2,4-triazole (propiconazole)

2-cyano-N-ethylcarbamoy-2-methoxyiminoacetamide (cymoxanil)

1-(4-chlorophenoxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)-2-butanone (triadimefon)

N-(trichloromethylthio)tetrahydrophthalimide (captan)

N-(trichloromethylthio)phthalimide (folpet)

1-[[[bis(4-fluorophenyl)][methyl]silyl]methyl]-1H-1,2,4-triazole.

NEMATOCIDES

S-methyl 1-(dimethylcarbamoyl)-N-(methylcarbamoyloxy)thioformimidate

S-methyl

1-carbamoyl-N-(methylcarbamoyloxy)thioformimidate

N-isopropylphosphoramidic acid, O-ethyl

O'-[4-(methylthio)-m-tolyl]diester (fenamiphos)

BACTERICIDES

tribasic copper sulfate

streptomycin sulfate

ACARICIDES

senecioic acid, ester with 2-sec-butyl-4,6-dinitrophenol (binapacryl)

6-methyl-1,3-cithiolo[4,5-α]quinoxalin-2-one (oxythioquinox)

ethyl 4,4'-dichlorobenzilate (chlorobenzilate)

1,1-bis(P-chlorophenyl)-2,2,2-trichloroethanol (dicofol)

bis(pentachloro-2,4-cyclopentadien-1-yl) (dienochlor)

tricyclohexyltin hydroxide (cyhexatin)

trans-5-(4-chlorophenyl)-N-cyclohexyl-4-methyl-2-oxothiazolidine-3-carboxamide (hexythiazox)

amitraz

propargite

fenbutatin-oxide

BIOLOGICAL

Bacillus thuringiensis

Avermectin B.

UTILITY

The compounds of this invention exhibit activity against a wide spectrum of foliar and soil inhabiting arthropods which are pests of growing and stored agronomic crops, forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health. Those skilled in the art will recognize that not all compounds are equally effective against all pests but the compounds of this invention display activity against economically important agronomic, forestry, greenhouse, ornamental food and fiber product, stored product, and nursery pests, such as:

larvae of the order Lepidoptera including fall and beet armyworm and other Spodoptera spp., tobacco budworm, corn earworm and other Heliothis spp., European corn borer, navel orangeworm, stalk/stem borers and other pyralids, cabbage and soybean loopers and other loopers, codling moth, grape berry moth and other tortricids, black cutworm, spotted cutworm, other cutworms and other noctuids, diamondback moth, green cloverworm, velvetbean caterpillar, green cloverworm, pink bollworm, gypsy moth, and spruce budworm;

foliar feeding larvae and adults of the order Coleoptera including Colorado potato beetle, Mexican bean beetle, flea beetle, Japanese beetles, and other leaf beetles, boll weevil, rice water weevil, granary weevil, rice weevil and other weevil pests, and soil inhabiting insects such as Western corn rootworm and other Diabrotica spp., Japanese beetle, European chafer and other coleopteran grubs, and wireworms;

adults and larvae of the orders Hemiptera and Homoptera including tarnished plant bug and other plant bugs (miridae), aster leafhopper and other leafhoppers (cicadellidae), rice planthopper, brown planthopper, and other planthoppers (fulgoroidea), psylids, whiteflies (aleurodidae), aphids (aphidae), scales (coccidae and diaspididae), lace bugs (tingidae), stink bugs (pentatomidae), cinch bugs and other seed bugs (lygaeidae), cicadas (cicadidae), spittlebugs (cercopids), squash bugs (coreidae), red bugs and cotton stainers (pyrrhocoridae);

adults and larvae of the order acari (mites) including European red mite, two spotted spider mite, rust mites, McDaniel mite, and foliar feeding mites;

adults and immatures of the order Orthoptera including grasshoppers;

adults and immatures of the order Diptera including leafminers, midges, fruit flies (tephritidae), and soil maggots;

adults and immatures of the order Thysanoptera including onion thrips and other foliar feeding thrips.

The compounds are also active against economically important livestock, household, public and animal health pests such as:

insect pests of the order Hymenoptera including carpenter ants, bees, hornets, and wasps;

insect pests of the order Diptera including house files, stable flies, face flies, horn flies, blow flies, and other muscoid fly pests, horse flies, deer flies and other Brachycera, mosquitoes, black flies, biting midges, sand flies, sciarids, and other Nematocera;

insect pests of the order Orthoptera including cockroaches and crickets;

insect pests of the order Isoptera including the Eastern subterranean termite and other termites;

insect pests of the order Mallophaga and Anoplura including the head louse, body louse, chicken head louse and other sucking and chewing parasitic lice that attack man and animals;

insect pests of the order Siphonoptera including the cat flea, dog flea and other fleas.

The specific species for which control is exemplified are: fall armyworm, Spodoptera fruigiperda: tobacco budworm, Heliothis virescens; boll weevil, Anthonomus grandis: aster leafhopper, Macrosteles fascifrons; southern corn rootworm, Diabrotica undecimpunctata. The pest control protection afforded by these compounds of the present invention is not limited, however to these species.

APPLICATION

Arthropod pests are controlled and protection of agronomic crops, animal and human health is achieved by applying one or more of the Formula I compounds of this invention, in an effective amount, to the locus of infestation, to the area to be protected, or directly on the pests to be controlled. Because of the diversity of habitat and behavior of these arthropod pest species, many different methods of application are employed. A preferred method of application is by spraying with equipment that distributes the compound in the environment of the pests, on the foliage, animal, person, or premise, in the soil or animal, to the plant part that is infested or needs to be protected. Alternatively, granular formulations of these toxicant compounds can be applied to or incorporated into the soil.

Other methods of application can also be employed including direct and residual sprays, aerial, baits, eartags, boluses, foggers, aerosols, and many others. The compounds can be incorporated into baits that are consumed by the arthropods or in devices such as traps and the like which entice them to ingest or otherwise contact the compounds.

The compounds of this invention can be applied in their pure state, but most often application will be of a formulation comprising one or more compounds with suitable carriers, diluents, and surfactants and Possibly in combination with a food depending on the contemplated end use. A preferred method of application involves spraying a water dispersion or refined oil solution of the compounds. Combinations with spray oils, spray oil concentrations, and synergists such as piperonyl butoxide often enhance the efficacy of the compounds of Formula I.

The rate of application of the Formula I compounds required for effective control will depend on such factors as the species of arthropod to be controlled, the pest's life cycle, life stage, its size, location, time of year, host crop or animal, feeding behavior, mating behavior, ambient moisture, temperature, etc. In general, application rates of 0.05 to 2 kg of active ingredient per hectare are sufficient to provide large-scale effective control of pests in agronomic ecosystems under normal circumstances, but as little as 0.001 kg/hectare or as 1 much as 8 kg hectare may be required. For nonagronomic applications, effective use rates will range from about 0.1 to 5 mg/square foot but as little as about 0.01 mg/square foot or as much as 15 mg/square foot may be required.

The following Examples demonstrate the control efficacy of compounds of Formula I on specific pests; see Tables 1 to 10 for compound descriptions. Compounds followed by a dash in the percent mortality column were either not screened or had less than 80% mortality on the test species.

EXAMPLE 8 Fall Armyworm

Test units, each consisting of an 8-ounce plastic cup containing a layer of wheat germ diet, approximately 0.5 cm thick, were Prepared. Ten third-instar larvae of fall armyworm (Spodoptera frigiperda) were placed into each cup. Solutions of each of the test compounds (acetone/distilled water 75/25 solvent) were sprayed onto the cups, a single solution per set of three cups. Spraying was accomplished by passing the cups, on a conveyer belt, directly beneath a flat fan hydraulic nozzle which discharged the spray at a rate of 0.5 pounds of active ingredient per acre (about 0.55 kg/ha) at 30 p.s.i. The cups were then covered and held at 27° C. and 50% relative humidity for 72 hours, after which time readings were taken. The results are tabulated below.

    ______________________________________                                                Compound                                                                               % Mort.                                                         ______________________________________                                                1       100                                                                    2       100                                                                    3       100                                                                    4       100                                                                    5       100                                                                    6       --                                                                     7       100                                                                    8       100                                                                    9       100                                                                    10      100                                                                    11      100                                                                    12      100                                                                    13      100                                                                    14      100                                                                    15      100                                                                    16      100                                                                    17      100                                                                    18      67                                                                     19      60                                                                     20      47                                                                     21      100                                                                    22      87                                                                     23      100                                                                    24      87                                                                     25      100                                                                    26      100                                                                    27      100                                                                    28      --                                                                     29      100                                                                    30      100                                                                    31      --                                                                     32      --                                                                     33      --                                                                     34      100                                                                    35      --                                                                     36      100                                                                    37      100                                                                    38      100                                                                    39      87                                                                     40      93                                                                     41      73                                                                     42      100                                                                    43      100                                                                    44      100                                                                    45      100                                                                    46      100                                                                    47      100                                                                    48      87                                                                     49      80                                                                     50      80                                                                     51      100                                                                    52      --                                                                     53      --                                                                     54      100                                                                    55      100                                                                    56      --                                                                     57      80                                                                     58      --                                                                     59      80                                                                     60      47                                                                     61      100                                                                    62      100                                                                    63      60                                                                     64      --                                                                     65      --                                                                     66      100                                                                    67      100                                                                    68      100                                                                    69      100                                                                    70      --                                                                     71      40                                                                     72      100                                                                    73      93                                                                     74      27                                                                     75      20                                                                     76      --                                                                     77      100                                                                    78      20                                                                     79      40                                                                     80      --                                                                     81      87                                                                     82      33                                                                     83      80                                                                     84      60                                                                     85      80                                                                     86      --                                                                     87      --                                                                     88      73                                                                     89      --                                                                     90.sup.1                                                                               100                                                                    91      100                                                                    92      100                                                                    93      100                                                                    94      100                                                                    95      93                                                                     96      --                                                                     97      --                                                                     98      100                                                                    99      93                                                                     100     60                                                                     101     --                                                                     102     --                                                                     103     --                                                                     104     100                                                                    105     100                                                                    106     100                                                                    107     100                                                                    108     100                                                                    109     --                                                                     110     100                                                                    111     100                                                                    112     100                                                                    113     33                                                                     114     --                                                                     115     --                                                                     116     --                                                                     117     --                                                                     118     --                                                                     119     --                                                                     120     --                                                                     121     60                                                                     122     --                                                                     123     --                                                                     124     --                                                                     125     --                                                                     126     --                                                                     127     --                                                                     128     --                                                                     129     --                                                                     130     --                                                                     131     --                                                                     132     --                                                                     133     --                                                                     134     33                                                                     135     --                                                                     136     --                                                                     137     --                                                                     138     33                                                                     139     --                                                                     140     --                                                                     141     --                                                                     142     33                                                                     143     100                                                                    144     60                                                                     145     --                                                                     146     --                                                                     147     --                                                                     148     --                                                                     149     13                                                                     150     --                                                                     151     --                                                                     152     --                                                                     153     --                                                                     154     --                                                                     155     --                                                                     156     --                                                                     157     --                                                                     158     --                                                                     159     --                                                                     160     20                                                                     161     --                                                                     162     --                                                                     163     --                                                                     164     --                                                                     165     0                                                                      166     0                                                                      167     --                                                                     168     47                                                                     169     --                                                                     170     20                                                                     171     --                                                                     172     --                                                                     173     --                                                                     174     --                                                                     175     --                                                                     176     67                                                                     177     87                                                                     178     33                                                                     179     --                                                                     180     --                                                                     181     100                                                                    182     --                                                                     183     --                                                                     184     --                                                                     185     --                                                                     186     --                                                                     187     --                                                                     188     --                                                                     189     100                                                                    190     93                                                                     191     20                                                                     192     --                                                                     193     60                                                                     194     --                                                                     195     --                                                                     196     --                                                                     197     --                                                                     198     --                                                                     199     --                                                                     200     --                                                                     201     --                                                                     202     100                                                                    203     --                                                                     204     100                                                                    205     67                                                                     206     100                                                                    207     --                                                                     208     --                                                                     209     40                                                                     210     --                                                                     211     --                                                                     212     100                                                                    213     --                                                                     214     --                                                                     215     --                                                                     216     73                                                                     217     --                                                                     218     --                                                                     219     --                                                                     220     60                                                                     221     --                                                                     222     100                                                                    223     --                                                                     224     47                                                                     225     --                                                                     226     --                                                                     227     73                                                                     228     --                                                                     229     --                                                                     230     --                                                                     231     --                                                                     232     --                                                                     233     --                                                                     234     47                                                                     235     --                                                                     236     --                                                                     237     87                                                                     238     53                                                                     239     --                                                                     240     93                                                                     241     100                                                                    242     100                                                                    243     13                                                                     244     --                                                                     245     67                                                                     246     --                                                                     247     --                                                                     248     --                                                                     249     --                                                                     250     40                                                                     251     40                                                                     252     67                                                                     253     87                                                                     254     100                                                                    255     30                                                                     256     --                                                                     257     --                                                                     258     60                                                                     259     --                                                                     260     --                                                                     261     --                                                                     262     --                                                                     263     --                                                                     265     --                                                                     266     --                                                                     267     --                                                                     268     --                                                                     269     --                                                              ______________________________________                                          .sup.1 Test procedure was identical to that described except there was         only one test cup.                                                       

EXAMPLE 9 Tobacco Budworm

The test procedure of Example 8 was repeated for efficacy against third-instar larvae of the tobacco budworm (Heliothis virescens) except that mortality was assessed at 48 hours. The results are tabulated below.

    ______________________________________                                                Compound                                                                               % Mort.                                                         ______________________________________                                                1       100                                                                    2       100                                                                    3       73                                                                     4       100                                                                    5       93                                                                     6       --                                                                     7       100                                                                    8       100                                                                    9       100                                                                    10      100                                                                    11      100                                                                    12      100                                                                    13      100                                                                    14      100                                                                    15      100                                                                    16      100                                                                    17      100                                                                    18      100                                                                    19      40                                                                     20      67                                                                     21      100                                                                    22      --                                                                     23      --                                                                     24      13                                                                     25      100                                                                    26      100                                                                    27      100                                                                    28      47                                                                     29      87                                                                     30      73                                                                     31      --                                                                     32      --                                                                     33      --                                                                     34      --                                                                     35      0                                                                      36      93                                                                     37      100                                                                    38      100                                                                    39      73                                                                     40      100                                                                    41      73                                                                     42      100                                                                    43      87                                                                     44      100                                                                    45      100                                                                    46      100                                                                    47      73                                                                     48      33                                                                     49      --                                                                     50      60                                                                     51      --                                                                     52      --                                                                     53      --                                                                     54      100                                                                    55      100                                                                    56      --                                                                     57      --                                                                     58      --                                                                     59      100                                                                    60      --                                                                     61      40                                                                     62      --                                                                     63      0                                                                      64      --                                                                     65      --                                                                     66      100                                                                    67      100                                                                    68      87                                                                     69      100                                                                    70      93                                                                     71      --                                                                     72      100                                                                    73      60                                                                     74      --                                                                     75      --                                                                     76      --                                                                     77      100                                                                    78      20                                                                     79      --                                                                     80      --                                                                     81      --                                                                     82      --                                                                     83      --                                                                     84      --                                                                     85      --                                                                     86      --                                                                     87      --                                                                     88      60                                                                     89      --                                                                     90.sup.1                                                                               --                                                                     91      100                                                                    92      100                                                                    93      100                                                                    94      87                                                                     95      80                                                                     96      --                                                                     97      --                                                                     98      100                                                                    99      --                                                                     100     --                                                                     101     --                                                                     102     --                                                                     103     87                                                                     104     33                                                                     105     100                                                                    106     100                                                                    107     100                                                                    108     --                                                                     109     --                                                                     110     67                                                                     111     --                                                                     112     --                                                                     113     --                                                                     114     --                                                                     115     --                                                                     116     --                                                                     117     --                                                                     118     --                                                                     119     --                                                                     120     --                                                                     121     --                                                                     122     --                                                                     123     --                                                                     124     --                                                                     125     --                                                                     126     --                                                                     127     --                                                                     128     --                                                                     129     --                                                                     130     --                                                                     131     --                                                                     132     0                                                                      133     --                                                                     134     --                                                                     135     --                                                                     136     --                                                                     137     --                                                                     138     67                                                                     139     --                                                                     140     27                                                                     141     --                                                                     142     20                                                                     143     100                                                                    144     80                                                                     145     --                                                                     146     --                                                                     147     --                                                                     148     --                                                                     149     --                                                                     150     --                                                                     151     --                                                                     152     --                                                                     153     --                                                                     154     --                                                                     155     --                                                                     156     --                                                                     157     --                                                                     158     --                                                                     159     --                                                                     160     --                                                                     161     --                                                                     162     --                                                                     163     --                                                                     164     --                                                                     165     80                                                                     166     73                                                                     167     40                                                                     168     --                                                                     169     --                                                                     170     47                                                                     171     --                                                                     172     27                                                                     173     --                                                                     174     --                                                                     175     --                                                                     176     80                                                                     177     20                                                                     178     --                                                                     179     73                                                                     180     --                                                                     181     53                                                                     182     --                                                                     183     --                                                                     184     --                                                                     185     --                                                                     186     --                                                                     187     --                                                                     188     --                                                                     189     --                                                                     190     53                                                                     191     --                                                                     192     --                                                                     193     --                                                                     194     13                                                                     195     --                                                                     196     --                                                                     197     --                                                                     198     --                                                                     199     --                                                                     200     --                                                                     201     --                                                                     202     100                                                                    203     --                                                                     204     67                                                                     205     67                                                                     206     100                                                                    207     33                                                                     208     --                                                                     209     60                                                                     210     --                                                                     211     --                                                                     212     --                                                                     213     --                                                                     214     --                                                                     215     --                                                                     216     20                                                                     217     13                                                                     218     --                                                                     219     --                                                                     220     --                                                                     221     --                                                                     222     --                                                                     223     --                                                                     224     --                                                                     225     --                                                                     226     --                                                                     227     --                                                                     228     --                                                                     229     --                                                                     230     --                                                                     231     --                                                                     232     --                                                                     233     --                                                                     234     --                                                                     235     --                                                                     236     80                                                                     237     --                                                                     238     60                                                                     239     80                                                                     240     --                                                                     241     70                                                                     242     93                                                                     243     7                                                                      244     --                                                                     245     --                                                                     246     --                                                                     247     --                                                                     248     --                                                                     249     --                                                                     250     --                                                                     251     --                                                                     252     87                                                                     253     53                                                                     254     --                                                                     255     7                                                                      256     33                                                                     257     47                                                                     258     33                                                                     259     --                                                                     260     --                                                                     261     --                                                                     262     --                                                                     263     --                                                                     264     --                                                                     265     --                                                                     266     --                                                                     267     --                                                                     268     --                                                                     269     --                                                              ______________________________________                                    

EXAMPLE 10 Aster Leafhopper

Test units were prepared from a series of 12-ounce cups, each containing oat (Avena sativa) seedlings in a 1-inch layer of sterilized soil. The test units were sprayed with individual solutions of the below-listed compounds. After the oats had dried from being sprayed, between 10 and 15 adult aster leafhoppers (Mascrosteles fascifrons) were aspirated into each of the covered cups. The cups were held at 27° C. and 50% relative humidity for 48 hours, after which time mortality readings were taken. The following table depicts the activity of the compounds tested on aster leafhopper.

    ______________________________________                                                Compound                                                                               % Mort.                                                         ______________________________________                                                1       --                                                                     2       --                                                                     3       --                                                                     4       6                                                                      5       --                                                                     6       --                                                                     7       44                                                                     8       --                                                                     9       100                                                                    10      85                                                                     11      --                                                                     12      95                                                                     13      83                                                                     14      --                                                                     15      73                                                                     16      75                                                                     17      --                                                                     18      100                                                                    19      100                                                                    20      100                                                                    21      --                                                                     22      --                                                                     23      --                                                                     24      --                                                                     25      --                                                                     26      --                                                                     27      --                                                                     28      --                                                                     29      --                                                                     30      --                                                                     31      --                                                                     32      --                                                                     33      --                                                                     34      --                                                                     35      --                                                                     36      --                                                                     37      91                                                                     38      --                                                                     39      --                                                                     40      --                                                                     41      60                                                                     42      98                                                                     43      89                                                                     44      --                                                                     45      100                                                                    46      --                                                                     47      100                                                                    48      --                                                                     49      --                                                                     50      --                                                                     51      --                                                                     52      --                                                                     53      --                                                                     54      --                                                                     55      --                                                                     56      --                                                                     57      --                                                                     58      --                                                                     59      --                                                                     60      12                                                                     61      96                                                                     62      --                                                                     63      --                                                                     64      --                                                                     65      --                                                                     66      50                                                                     67      --                                                                     68      72                                                                     69      88                                                                     70      84                                                                     71      --                                                                     72      --                                                                     73      --                                                                     74      --                                                                     75      --                                                                     76      --                                                                     77      100                                                                    78      83                                                                     79      71                                                                     80      --                                                                     81      100                                                                    82      --                                                                     83      82                                                                     84      --                                                                     85      --                                                                     86      --                                                                     87      --                                                                     88      91                                                                     89      --                                                                     90.sup.1                                                                               --                                                                     91      --                                                                     92      77                                                                     93      94                                                                     94      --                                                                     95      74                                                                     96      --                                                                     97      --                                                                     98      --                                                                     99      100                                                                    100     --                                                                     101     --                                                                     102     --                                                                     103     --                                                                     104     --                                                                     105     100                                                                    106     84                                                                     107     100                                                                    108     71                                                                     109     --                                                                     110     --                                                                     111     --                                                                     112     --                                                                     113     --                                                                     114     --                                                                     115     --                                                                     116     --                                                                     117     --                                                                     118     --                                                                     119     --                                                                     120     --                                                                     121     --                                                                     122     --                                                                     123     --                                                                     124     --                                                                     125     --                                                                     126     --                                                                     127     --                                                                     128     --                                                                     129     --                                                                     130     --                                                                     131     --                                                                     132     --                                                                     133     --                                                                     134     --                                                                     135     --                                                                     136     --                                                                     137     --                                                                     138     92                                                                     139     --                                                                     140     --                                                                     141     --                                                                     142     --                                                                     143     --                                                                     144     --                                                                     145     --                                                                     146     --                                                                     147     --                                                                     148     --                                                                     149     --                                                                     150     --                                                                     151     --                                                                     152     --                                                                     153     --                                                                     154     --                                                                     155     --                                                                     156     --                                                                     157     --                                                                     158     --                                                                     159     --                                                                     160     --                                                                     161     --                                                                     162     --                                                                     163     --                                                                     164     --                                                                     165     36                                                                     166     --                                                                     167     --                                                                     168     --                                                                     169     --                                                                     170     --                                                                     171     --                                                                     172     --                                                                     173     --                                                                     174     --                                                                     175     --                                                                     176     91                                                                     177     93                                                                     178     60                                                                     179     --                                                                     180     --                                                                     181     98                                                                     182     68                                                                     183     --                                                                     184     --                                                                     185     --                                                                     186     --                                                                     187     --                                                                     188     --                                                                     189     81                                                                     190     70                                                                     191     --                                                                     192     95                                                                     193     --                                                                     194     --                                                                     195     --                                                                     196     --                                                                     197     --                                                                     198     --                                                                     199     --                                                                     200     --                                                                     201     --                                                                     202     100                                                                    203     --                                                                     204     94                                                                     205     --                                                                     206     66                                                                     207     57                                                                     208     --                                                                     209     --                                                                     210     90                                                                     211     --                                                                     212     88                                                                     213     --                                                                     214     --                                                                     215     --                                                                     216     --                                                                     217     --                                                                     218     --                                                                     219     --                                                                     220     --                                                                     221     --                                                                     222     --                                                                     223     --                                                                     224     --                                                                     225     --                                                                     226     --                                                                     227     --                                                                     228     --                                                                     229     --                                                                     230     --                                                                     231     --                                                                     232     --                                                                     233     --                                                                     234     92                                                                     235     100                                                                    236     91                                                                     237     98                                                                     238     98                                                                     239     98                                                                     240     100                                                                    241     97                                                                     242     --                                                                     243     --                                                                     244     --                                                                     245     --                                                                     246     --                                                                     247     --                                                                     248     --                                                                     249     --                                                                     250     --                                                                     251     --                                                                     252     --                                                                     253     --                                                                     254     --                                                                     255     --                                                                     256     --                                                                     257     --                                                                     258     62                                                                     259     --                                                                     260     --                                                                     261     --                                                                     262     --                                                                     263     --                                                                     264     --                                                                     265     --                                                                     266     --                                                                     267     --                                                                     268     --                                                                     269     --                                                              ______________________________________                                    

EXAMPLE 11 Southern Corn Rootworm

Test units, each consisting of an 8-ounce plastic cup containing 1 sprouted corn seed, were prepared. Sets of three tests units were sprayed as described in Example 8 with individual solutions of the below-listed compounds. After the spray on the cups had dried, five third-instar larvae of the southern corn rootworm (Diabrotica undecimpunctata howardi) were placed into each cup. A moistened dental wick was inserted into each cup to prevent drying and the cups were then covered. The cups were then held at 27° C. and 50% relative humidity for 48 hours, after which time mortality readings were taken. The results are tabulated below.

    ______________________________________                                                Compound                                                                               % Mort.                                                         ______________________________________                                                1       100                                                                    2       100                                                                    3       100                                                                    4       100                                                                    5       100                                                                    6       --                                                                     7       100                                                                    8       100                                                                    9       100                                                                    10      100                                                                    11      100                                                                    12      100                                                                    13      100                                                                    14      100                                                                    15      100                                                                    16      100                                                                    17      100                                                                    18      100                                                                    19      100                                                                    20      100                                                                    21      100                                                                    22      --                                                                     23      100                                                                    24      93                                                                     25      --                                                                     26      87                                                                     27      --                                                                     28      --                                                                     29      --                                                                     30      87                                                                     31      100                                                                    32      --                                                                     33      --                                                                     34      100                                                                    35      --                                                                     36      100                                                                    37      100                                                                    38      100                                                                    39      100                                                                    40      80                                                                     41      100                                                                    42      100                                                                    43      100                                                                    44      100                                                                    45      --                                                                     46      100                                                                    47      --                                                                     48      --                                                                     49      --                                                                     50      47                                                                     51      100                                                                    52      --                                                                     53      --                                                                     54      100                                                                    55      100                                                                    56      --                                                                     57      --                                                                     58      30                                                                     59      100                                                                    60      80                                                                     61      100                                                                    62      100                                                                    63      80                                                                     64      100                                                                    65      --                                                                     66      100                                                                    67      100                                                                    68      100                                                                    69      100                                                                    70      100                                                                    71      47                                                                     72      73                                                                     73      --                                                                     74      100                                                                    75      67                                                                     76      67                                                                     77      100                                                                    78      --                                                                     79      100                                                                    80      --                                                                     81      100                                                                    82      100                                                                    83      100                                                                    84      --                                                                     85      --                                                                     86      --                                                                     87      93                                                                     88      100                                                                    89      100                                                                    90.sup.1                                                                               --                                                                     91      100                                                                    92      100                                                                    93      100                                                                    94      100                                                                    95      100                                                                    96      100                                                                    97      100                                                                    98      100                                                                    99      100                                                                    100     100                                                                    101     100                                                                    102     40                                                                     103     --                                                                     104     --                                                                     105     100                                                                    106     67                                                                     107     100                                                                    108     100                                                                    109     --                                                                     110     100                                                                    111     100                                                                    112     100                                                                    113     --                                                                     114     --                                                                     115     --                                                                     116     --                                                                     117     --                                                                     118     --                                                                     119     --                                                                     120     --                                                                     121     --                                                                     122     --                                                                     123     --                                                                     124     --                                                                     125     --                                                                     126     --                                                                     127     --                                                                     128     --                                                                     129     --                                                                     130     60                                                                     131     --                                                                     132     --                                                                     133     47                                                                     134     100                                                                    135     --                                                                     136     100                                                                    137     100                                                                    138     100                                                                    139     100                                                                    140     93                                                                     141     100                                                                    142     --                                                                     143     100                                                                    144     100                                                                    145     87                                                                     146     --                                                                     147     100                                                                    148     47                                                                     149     --                                                                     150     --                                                                     151     --                                                                     152     100                                                                    153     --                                                                     154     --                                                                     155     --                                                                     156     --                                                                     157     --                                                                     158     --                                                                     159     --                                                                     160     0                                                                      161     --                                                                     162     --                                                                     163     --                                                                     164     93                                                                     165     100                                                                    166     87                                                                     167     --                                                                     168     100                                                                    169     100                                                                    170     100                                                                    171     --                                                                     172     93                                                                     173     100                                                                    174     --                                                                     175     --                                                                     176     100                                                                    177     100                                                                    178     100                                                                    179     100                                                                    180     100                                                                    181     100                                                                    182     100                                                                    183     60                                                                     184     --                                                                     185     100                                                                    186     100                                                                    187     --                                                                     188     --                                                                     189     100                                                                    190     100                                                                    191     100                                                                    192     100                                                                    193     100                                                                    194     100                                                                    195     --                                                                     196     --                                                                     197     --                                                                     198     --                                                                     199     --                                                                     200     --                                                                     201     --                                                                     202     100                                                                    203     --                                                                     204     100                                                                    205     100                                                                    206     100                                                                    207     93                                                                     208     100                                                                    209     100                                                                    210     100                                                                    211     100                                                                    212     100                                                                    213     --                                                                     214     --                                                                     215     --                                                                     216     --                                                                     217     --                                                                     218     --                                                                     219     --                                                                     220     --                                                                     221     --                                                                     222     --                                                                     223     --                                                                     224     100                                                                    225     --                                                                     226     --                                                                     227     100                                                                    228     13                                                                     229     --                                                                     230     --                                                                     231     --                                                                     232     --                                                                     233     --                                                                     234     100                                                                    235     100                                                                    236     100                                                                    237     100                                                                    238     100                                                                    239     100                                                                    240     100                                                                    241     100                                                                    242     100                                                                    243     --                                                                     244     --                                                                     245     27                                                                     246     --                                                                     247     --                                                                     248     --                                                                     249     --                                                                     250     --                                                                     251     --                                                                     252     100                                                                    253     100                                                                    254     80                                                                     255     100                                                                    256     --                                                                     257     93                                                                     258     100                                                                    259     --                                                                     260     93                                                                     261     --                                                                     262     --                                                                     263     --                                                                     264     --                                                                     265     --                                                                     266     --                                                                     267     --                                                                     268     --                                                                     269     --                                                              ______________________________________                                    

EXAMPLE 12 Boll Weevil

Five adult boll weevils (Anthonomus grandis) were placed into each of a series of 9-ounce cups. The test procedure employed was then otherwise the same as in Example 8 with three cups per treatment. Mortality readings were taken 48 hours after treatment. The results are tabulated below.

    ______________________________________                                                Compound                                                                               % Mort.                                                         ______________________________________                                                1       87                                                                     2       66                                                                     3       20                                                                     4       100                                                                    5       80                                                                     6       --                                                                     7       100                                                                    8       --                                                                     9       100                                                                    10      100                                                                    11      100                                                                    12      100                                                                    13      100                                                                    14      100                                                                    15      100                                                                    16      100                                                                    17      100                                                                    18      100                                                                    19      100                                                                    20      100                                                                    21      100                                                                    22      93                                                                     23      100                                                                    24      100                                                                    25      --                                                                     26      --                                                                     27      --                                                                     28      --                                                                     29      100                                                                    30      100                                                                    31      100                                                                    32      --                                                                     33      --                                                                     34      100                                                                    35      --                                                                     36      87                                                                     37      100                                                                    38      73                                                                     39      87                                                                     40      100                                                                    41      100                                                                    42      100                                                                    43      100                                                                    44      93                                                                     45      93                                                                     46      93                                                                     47      100                                                                    48      80                                                                     49      67                                                                     50      80                                                                     51      93                                                                     52      --                                                                     53      --                                                                     54      100                                                                    55      --                                                                     56      --                                                                     57      53                                                                     58      --                                                                     59      100                                                                    60      --                                                                     61      100                                                                    62      100                                                                    63      100                                                                    64      100                                                                    65      --                                                                     66      100                                                                    67      100                                                                    68      100                                                                    69      93                                                                     70      53                                                                     71      --                                                                     72      40                                                                     73      87                                                                     74      100                                                                    75      60                                                                     76      93                                                                     77      100                                                                    78      100                                                                    79      100                                                                    80      --                                                                     81      100                                                                    82      100                                                                    83      100                                                                    84      100                                                                    85      80                                                                     86      --                                                                     87      100                                                                    88      100                                                                    89      100                                                                    90.sup.1                                                                               --                                                                     91      93                                                                     92      100                                                                    93      100                                                                    94      100                                                                    95      100                                                                    96      73                                                                     97      67                                                                     98      100                                                                    99      100                                                                    100     100                                                                    101     100                                                                    102     40                                                                     103     --                                                                     104     --                                                                     105     100                                                                    106     100                                                                    107     100                                                                    108     100                                                                    109     --                                                                     110     100                                                                    111     100                                                                    112     100                                                                    113     7                                                                      114      --                                                                    115     --                                                                     116     --                                                                     117     --                                                                     118     --                                                                     119     --                                                                     120     --                                                                     121     --                                                                     122     67                                                                     123     --                                                                     124     --                                                                     125     --                                                                     126     --                                                                     127     --                                                                     128     --                                                                     129     --                                                                     130     --                                                                     131     --                                                                     132     --                                                                     133     100                                                                    134     93                                                                     135     --                                                                     136     --                                                                     137     93                                                                     138     100                                                                    139     47                                                                     140     93                                                                     141     93                                                                     142     --                                                                     143     100                                                                    144     100                                                                    145     --                                                                     146     60                                                                     147     93                                                                     148     67                                                                     149     0                                                                      150     --                                                                     151     --                                                                     152     --                                                                     153     --                                                                     154     --                                                                     155     --                                                                     156     --                                                                     157     --                                                                     158     --                                                                     159     --                                                                     160     33                                                                     161     --                                                                     162     --                                                                     163     33                                                                     164     73                                                                     165     100                                                                    166     80                                                                     167     13                                                                     168     93                                                                     169     87                                                                     170     100                                                                    171     --                                                                     172     --                                                                     173     20                                                                     174     --                                                                     175     --                                                                     176     100                                                                    177     100                                                                    178     73                                                                     179     --                                                                     180     --                                                                     181     100                                                                    182     87                                                                     183     100                                                                    184     --                                                                     185     87                                                                     186     73                                                                     187     --                                                                     188     --                                                                     189     100                                                                    190     93                                                                     191     100                                                                    192     100                                                                    193     100                                                                    194     60                                                                     195     --                                                                     196     --                                                                     197     --                                                                     198     --                                                                     199     --                                                                     200     --                                                                     201     --                                                                     202     100                                                                    203     --                                                                     204     100                                                                    205     100                                                                    206     100                                                                    207     87                                                                     208     100                                                                    209     100                                                                    210     93                                                                     211     100                                                                    212     100                                                                    213     --                                                                     214     --                                                                     215     --                                                                     216     100                                                                    217     --                                                                     218     --                                                                     219     --                                                                     220     --                                                                     221     --                                                                     222     --                                                                     223     --                                                                     224     --                                                                     225     --                                                                     226     --                                                                     227     87                                                                     228     --                                                                     229     --                                                                     230     --                                                                     231     --                                                                     232     --                                                                     233     --                                                                     234     --                                                                     235     33                                                                     236     80                                                                     237     --                                                                     238     --                                                                     239     --                                                                     240     93                                                                     241     --                                                                     242     100                                                                    243     --                                                                     244     --                                                                     245     27                                                                     246     --                                                                     247     --                                                                     248     --                                                                     249     --                                                                     250     --                                                                     251     --                                                                     252     100                                                                    253     100                                                                    254     100                                                                    255     93                                                                     256     100                                                                    257     87                                                                     258     93                                                                     259     --                                                                     260     --                                                                     261     --                                                                     262     20                                                                     263     --                                                                     264     --                                                                     265     --                                                                     266     --                                                                     267     --                                                                     268     --                                                                     269     --                                                              ______________________________________                                     

What is claimed is:
 1. A compound of the formula ##STR28## wherein: Q is ##STR29## A is O, S(O)_(q) or NR₇ ; R₁ and R₂ are independently R₈, halogen, CN, NO₂, N₃, SCN, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, C(O)R₈, CO₂ R₈, C(O)NR₈ R₉, OC(O)R₈, OCO₂ R₈, OC(O)NR₈ R₉, NR₉ C(O)R₈, NR₉ C(O)NR₈ R₉, OSO₂ R₈, NR₉ SO₂ R₈, or when m is 2, R₁ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O or CH₂ CH₂ O each of which is optionally substituted with 1 to 4 halogen atoms or 1 to 2 methyl groups, or when n is 2, R₂ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O or CH₂ CH₂ O each of which can be substituted 1 to 4 halogens or 1 to 2 methyl groups;R₃ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₄ -C₆ alkylcycloalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylakyl, OR₈, S(O)_(q) R₈, NR₈ R₉, CN, CO₂ R₈, C(O)R₈, C(O)NR₈ R₉, C(S)NR₈ R₉, C(S)R₈, C(S)SR₈, phenyl optionally substituted with (R₁₀)_(p) or benzyl optionally substituted with 1 to 3 substituents independently selected from W or R₃ is C₃ -C₆ cycloalkyl optionally substituted with 1 to 2 halogens or 1 to 2 CH₃ ; R₄ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ cyanoalkyl, phenyl optionally substituted with (R₁₀)_(p) or benzyl optionally substituted with 1 to 3 substituents independently selected from W; R₅ and R₆ are independently H, C₁ -C₂₂ alkyl, C₂ -C₂₂ alkoxyalkyl, C₂ -C₂₂ alkylcarbonyl, C₂ -C₂₂ alkoxycarbonyl, C₂ -C₂₂ haloalkyl carbonyl, C₂ -C₂₂ haloalkoxycarbony, SR₁₁, CHO, C₁ -C₄ alkylsulfonyl, phenylsulfonyl optionally substituted with 1 to 3 substituents independently selected from W; C₇ -C₁₅ phenoxycarbonyl optionally substituted with 1 to 3 substituents selected from W; C₇ -C₁₅ phenylcarbonyl optionally substituted with 1 to 3 substituents independently selected from W; C(O)CO₂ C₁ to C₄ alkyl, C₈ -C₁₂ benzyloxycarbonyl optionally substituted with 1 to 3 substituents independently selected from W; or R₅ and R₆ are independently phenyl optionally substituted with 1 to 3 substituents independently selected from W, or benzyl optionally substituted with 1 to 3 substituents independently selected from W; R₇ is H, C₁ -C₄ alkyl or phenyl optionally substituted with W; SR₈, SOR₈, SO₂ R₈, C(O)R₈, CO₂ R₈, C(O)NR₈ R₉, C(S)NR₈ R₉, C(S)R₈, C(S)OR₈, P(O)(OR₈)₂, P(S)(OR₈)₂, P(O)(R₃)OR₈ or P(O)(R₈)SR₈ ; provided that when R₇ is other than COR₈, C(O)NR₈ R₉ or C(S)NR₈ R₉ then R₈ is other than H; R₈ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₄ -C₇ cycloalkylalkyl C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ alkylthioalkyl, C₁ -C₆ nitroalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₃ -C₆ cycloalkyl, C₃ -C₆ halocycloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W or benzyl optionally substituted with 1 to 3 substituents independently selected from W; R₉ is H, C₁ -C₄ alkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, or R₈ and R₉ is optionally taken together as (CH₂)₄, (CH₂)₅ or (CH₂ CH₂ OCH₂ CH₂); R₁₀ is R₈, halogen, CN, NO₂, N₃, SCN, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, COR₈, CO₂ R₈, CONR₈ R₉, SO₂ NR₈ R₉, OC(O)R₈, OCO₂ R₈, OC(O)NR₈ R₉, NR₉ C(O)R₈, NR₉ C(O)NR₈ R₉, OSO₂ R₈, NR₉ SO₂ R₈ or when p is 2, R₁₀ is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O, or CH₂ CH₂ O each of which is optionally substituted with independently, 1 to 4 halogen atoms or 1 to 2 methyl groups; R₁₁ is C₁ -C₂₂ alkyl, C₁ -C₂₂ haloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W, or R₁₁ is NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, NR₁₂ R₁₆, SR₁₄, ##STR30## R₁₂ and R₁₆ are independently selected from C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₃ -C₆ cycloalkyl, C₄ -C₇ cylcoalkylalkyl, C₂ -C₆ cyanoalkyl, C₂ -C₆ alkoxyalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₄ -C₈ dialkylaminocarbonylalkyl, phenyl optionally substituted by 1 to 2 substituents selected from W, benzyl optionally substituted by 1 to 2 substituents selected from W and phenethyl optionally substituted by 1 to 2 substituents selected from W, or R₁₂ -R₁₆ is optionally taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂, each ring optionally substituted with 1 to 2 CH₃ ; R₁₃ is F, C₁ -C₂₀ alkyl, C₁ -C₆ haloalkyl, C₂ -C₈ dialkylamino, piperidinyl, pyrrolidinyl, morpholinyl, phenyl optionally substituted with 1 to 3 substituents selected from W, or R₁₃ is C₁ -C₂₀ alkoxy C₁ -C₆ haloalkoxy or C₁ -C₄ alkoxy substituted with cyano, nitro, C₁ -C₄ alkoxy, C₄ -C₈ alkoxyalkoxy, C₁ -C₂ alkylthio, C₂ -C₃ alkoxycarbonyl, C₃ -C₅ dialkylaminocarbonyl or phenyl optionally substituted with 1 to 3 substituents independently selected from W, or R₁₃ is phenoxy optionally substituted with 1 to 3 substituents selected from W; R₁₄ and R₁₅ are independently selected from C₁ -C₄ alkyl, C₂ -C₄ haloalkyl, phenyl optionally substituted with 1 to 3 substituents independently selected from W or R₁₄ and R₁₅ is optionally taken together as (CH₂)₂, (CH₂)₃ or CH₂ C(CH₃)₂ CH₂ ; W is halogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂ haloalkyl, C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl; m is 1 to 5; n is 1 to 4; q is 0 to 2; p is 1 to 3; a is 0 to 2; X is O or S; Y is O or S; and Z is O or S.
 2. A compound according to claim 1 wherein: when R₃ or R₄ is H and A is oxygen then the remaining R₃ or R₄ is other than phenyl or phenyl optionally substituted with W.
 3. A compound according to claim 1 wherein:R₁, R₂ and R₁₀ are R₈, halogen, CN, NO₂, OR₈, SR₈, SOR₈, SO₂ R₈, NR₈ R₉, CO₂ R₈, SO₂ NR₈ R₉, or when m, n or q is 2, then R₁, R₂ or R₁₀ respectively is optionally taken together to form a 5 or 6 membered fused ring as OCH₂ O, OCH₂ CH₂ O or CH₂ CH₂ O each of which is optionally substituted with 1 to 4 halogens or 1 to 2 methyl groups; R₈ is H, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₃ -C₆ cycloalkylalkyl, C₃ -C₆ halocycloalkylalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₃ -C₆ cycloalkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W or benzyl optionally substituted with 1 to 2 substituents independently selected from W; R₅ and R₆ are independently H, C₁ -C₃ alkyl, C₂ -C₄ alkylcarbonyl, C₂ -C₄ alkoxycarbonyl, CHO, SR₁₁, phenyl optionally substituted with 1 to 2 substituents independently selected from W, or benzyl optionally substituted with 1 to 2 substituents independently selected from W; R₁₁ is C₁ -C₃ alkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W, NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, NR₁₂ R₁₆, ##STR31## R₁₂ and R₁₆ are independently selected from C₁ -C₆ alkyl, C₁ -C₆ haloalkyl, C₅ -C₆ cycloalkyl, C₃ -C₈ alkoxycarbonyl- alkyl, phenyl, benzyl and phenethyl or each phenyl, benzyl and phenethyl optionally substituted with 1 to 2 substituents independently selected from W, or R₁₂ and R₁₆ can be taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ; R₁₄ and R₁₅ are independently selected from C₁ to C₃ alkyl or phenyl; m is 1 to 2; n is 1 to 2; p is 1 to 2; q is 0; and a is
 2. 4. A compound according to claim 3 wherein:R₃ is H, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, CN, phenyl optionally substituted with (R₁₀)_(p) or benzyl optionally substituted with 1 to 2 substituents independently selected from W; R₄ is H, C₁ -C₃ alkyl, C₃ -C₄ alkenyl or C₃ -C₄ alkynyl; R₅ is H, Me, CO₂ Me, CO₂ Et, SR₁₁ or phenyl optionally substituted with 1 to 2 substituents independently selected from W; R₆ is H, Me, C(O)Me, CO₂ Me or SR₁₁ ; R₁₁ is C₁ -C₃ alkyl, NR₁₂ C(O)R₁₃, NR₁₂ S(O)_(a) R₁₃, C(O)R₁₃, or phenyl optionally substituted with Cl, NO₂ or CH₃ ; R₁₂ is C₁ -C₄ alkyl or phenyl optionally substituted with Cl or CH3; R₁₃ is C₁ -C₁₂ alkyl, C₁ -C₁₂ alkoxy, C₁ -C₆ haloalkyl, dimethylamino, phenyl optionally substituted with Cl or CH₃, or R₁₃ is C₁ -C₄ alkoxy substituted with C₂ -C₄ alkoxy or 1 to 6 halogens; R₇ is H, C₁ -C₄ alkyl, C₂ -C₄ alkenyl, C₂ -C₄ alkynyl, C₂ -C₄ alkylcarbonyl, C₂ -C₄ alkoxycarbonyl or C₁ -C₄ alkylsulfonyl.
 5. A compound according to claim 4 wherein:R₁ and R₂ are independently selected from F, Cl, Br, CN, NO₂, OMe, CF₃, OCF₂ H, OCF₂ CF₂ H, SMe, SO₂ Me, SCF₂ H or when m or n is 2 R₁ or R₂ respectively is optionally taken together as CH₂ C(CH₃)₂ O or CF₂ CF₂ O; R₃ is C₁ to C₄ alkyl, allyl, propargyl, or phenyl optionally substituted with F, Cl, Br, CF₃, OCF₂ H, OCF₃, SCF₂ H, CN, NO₂, CH₃, OMe or CO₂ Me; R₄ is H or CH₃ ; R₅ is H, CH₃ CO₂ CH₃, CO₂ Et, or phenyl optionally substituted with F or Cl; R₆ is H, CH₃, C(O)CH₃ or CO₂ CH₃ ; and A is O.
 6. A compound according to claim 5:2-[6-chloro-2,3-dihydro-2-methyl-2-(2-propenyl)-3-benzo-furanylidene]-N-[4-(trifluoromethoxy)phenyl]hydrazine carboxamide.
 7. An arthropodicidal composition comprising an arthropodicidally effective amount of a compound according to claim 1 and a carrier therefor.
 8. A method for controlling arthropods comprising applying to them or to their environment an arthropodicidally effective amount of a compound according to claim
 1. 